Search Result
Results for "Acetylcholine Transporters Inhibitors" in MCE Product Catalog:
7951
Inhibitors & Agonists
12
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-B0282
-
-
- HY-B1813A
-
|
(±)-Vesamicol hydrochloride
(±)-AH5183 hydrochloride
|
Sigma Receptor
|
Neurological Disease
|
|
(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively.
|
-
- HY-101086
-
-
- HY-N7506
-
|
13-Hydroxyisobakuchiol
Delta3,2-Hydroxylbakuchiol
|
Monoamine Transporter
Dopamine Transporter
|
Neurological Disease
|
|
Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) isolated from Psoralea corylifolia (L.), is a potent monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50=0.58 μM) and norepinephrine transporter (NET) (IC50=0.69 μM) than for the serotonin transporter (SERT) (IC50=312.02 μM). 13-Hydroxyisobakuchiol has the potential for the research of disorders such as Parkinson's disease, depression, and cocaine addiction.
|
-
- HY-U00439
-
-
- HY-W010936
-
|
Nitrobenzylthioinosine
NBMPR
|
Adenosine Receptor
|
Neurological Disease
|
|
Nitrobenzylthioinosine is an ENT1 transporter inhibitor that binds to ENT1 transporter with high affinity. Nitrobenzylthioinosine is a photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine can cross the blood-brain barrier.
|
-
- HY-18728
-
-
- HY-16771
-
-
- HY-109031
-
|
Dotinurad
|
URAT1
|
Metabolic Disease
|
|
Dotinurad is a potent and selective urate reabsorption inhibitor. Dotinurad inhibits urate transporter 1 (URAT1) with an IC50 value of 37.2 nM. Dotinurad acts as a uricosuric agent.
|
-
- HY-B1274
-
-
- HY-101315
-
|
AHN 1-055 hydrochloride
3α-Bis-(4-fluorophenyl) Methoxytropane hydrochloride
|
Dopamine Transporter
|
Neurological Disease
|
|
AHN 1-055 hydrochloride is a dopamine uptake inhibitor, with an IC50 of 71 nM. AHN 1-055 hydrochloride binds with high affinity to the dopamine transporter (DAT) and may serve as leads for the development of agentia to treat cocaine abuse.
|
-
- HY-B1552B
-
-
- HY-136146
-
|
SUVN-911
|
nAChR
|
Neurological Disease
|
|
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
|
-
- HY-W011391
-
|
GPNA hydrochloride
|
Apoptosis
|
Cancer
|
|
GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na +-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na +-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells.
|
-
- HY-B0379A
-
|
Adiphenine hydrochloride
|
nAChR
|
Neurological Disease
|
|
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 µM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has narcotic and anticonvulsant effects.
|
-
- HY-101372A
-
|
Oxotremorine M iodide
|
mAChR
|
Neurological Disease
|
|
Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms.
|
-
- HY-B1704A
-
-
- HY-B2246A
-
|
D-Carnitine hydrochloride
(S)-Carnitine hydrochloride
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-Carnitine hydrochloride ((S)-Carnitine Hydrochloride) has been used to study sulfur factor transporter SLC22A4 and carnitine transporter SLC22A5 in ergot. D-Carnitine hydrochloride is also used to get palmitic acid into mitochondria.
|
-
- HY-B0321
-
|
Tropicamide
Ro 1-7683
|
mAChR
|
Neurological Disease
|
|
Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops.
|
-
- HY-109043A
-
|
Solriamfetol hydrochloride
JZP-110 hydrochloride; ADX-N05 hydrochloride; R228060 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Solriamfetol hydrochloride (JZP-110 hydrochloride) is an orally active and selective dopamine and norepinephrine reuptake inhibitor with IC50s of 2.9 μM and 4.4 μM for dopamine and norepinephrine transporters, respectively. Solriamfetol hydrochloride has robust wake-promoting effects.
|
-
- HY-109043
-
|
Solriamfetol
JZP-110; ADX-N05; R228060
|
Dopamine Receptor
|
Neurological Disease
|
|
Solriamfetol (JZP-110) is an orally active and selective dopamine and norepinephrine reuptake inhibitor with IC50s of 2.9 μM and 4.4 μM for dopamine and norepinephrine transporters, respectively. Solriamfetol has robust wake-promoting effects.
|
-
- HY-N4080
-
|
Cyclobuxine D
|
mAChR
|
Inflammation/Immunology
|
|
Cyclobuxine D is a steroidal alkaloid extracted from Buxus microphylla. Cyclobuxine D has a significant bradycardic effect in the rat heart and an inhibitory action on acetylcholine and Ba ++−induced contraction of the longitudinal muscle isolated from the rabbit jejunum.
|
-
- HY-N0455
-
|
L-Arginine
(S)-(+)-Arginine
|
NO Synthase
Endogenous Metabolite
|
Cardiovascular Disease
|
|
L-Arginine ((S)-(+)-Arginine) is the substrate for the endothelial nitric oxide synthase (eNOS) to generate NO. L-Arginine is transported into vascular smooth muscle cells by the cationic amino acid transporter family of proteins where it is metabolized to nitric oxide (NO), polyamines, or L-proline.
|
-
- HY-107416
-
|
RHC 80267
U-57908
|
Acyltransferase
mAChR
COX
Phospholipase
|
Metabolic Disease
Neurological Disease
|
|
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).
|
-
- HY-100234A
-
-
- HY-100234
-
-
- HY-109019
-
|
Vorolanib
CM082; X-82
|
VEGFR
PDGFR
|
Cancer
Cardiovascular Disease
|
|
Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).
|
-
- HY-19752A
-
|
VU0357017 hydrochloride
CID-25010775
|
mAChR
|
Neurological Disease
|
|
VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia.
|
-
- HY-P1271
-
|
Catestatin
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
|
-
- HY-P1271A
-
|
Catestatin TFA
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
|
-
- HY-107641
-
|
α-Cyano-4-hydroxycinnamic acid
α-Cyano-4-hydroxycinnamate
|
Monocarboxylate Transporter
|
Metabolic Disease
|
|
α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications.
|
-
- HY-17590
-
-
- HY-12641
-
|
Pyrantel tartrate
|
Parasite
Antibiotic
|
Infection
|
|
Pyrantel tartrate, a tetrahydropyrimidine anthelmintic, and is a nicotinic acetylcholine receptor (nAChR) agonist. Pyrantel tartrate can elicit spastic muscle paralysis in parasitic worms. Pyrantel tartrate can be used for the research of astrointestinal nematodes infections.
|
-
- HY-100017
-
|
BAY-876
|
GLUT
|
Cancer
|
|
BAY-876 is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC50 of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth.
|
-
- HY-N7433
-
-
- HY-W020468
-
|
Linopirdine
DuP 996
|
Potassium Channel
TRP Channel
|
Neurological Disease
|
|
Linopirdine (DuP 996) is an orally active, selective M-type K + current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue.
|
-
- HY-12640
-
|
Pyrantel pamoate
Pyrantel embonate
|
Parasite
Antibiotic
|
Infection
|
|
Pyrantel pamoate (Pyrantel embonate), a tetrahydropyrimidine anthelmintic, and is a nicotinic acetylcholine receptor (nAChR) agonist. Pyrantel pamoate can elicit spastic muscle paralysis in parasitic worms. Pyrantel pamoate can be used for the research of astrointestinal nematodes infections.
|
-
- HY-131005
-
-
- HY-B1272
-
-
- HY-16736A
-
-
- HY-18638
-
|
TCID
4,5,6,7-Tetrachloroindan-1,3-dione
|
Deubiquitinase
|
Neurological Disease
|
|
TCID (4,5,6,7-Tetrachloroindan-1,3-dione) is a potent and selective neuronal ubiquitin C-terminal hydrolase (UCH-L3) inhibitor with an IC50 of 0.6 μM. TCID diminishes glycine transporter GlyT2 ubiquitination in brainstem and spinal cord primary neurons.
|
-
- HY-110160
-
|
Pozanicline dihydrochloride
ABT-089 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant.
|
-
- HY-112683
-
|
V-9302
|
Others
|
Cancer
|
|
V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5). V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
|
-
- HY-112683A
-
|
V-9302 hydrochloride
|
Others
|
Cancer
|
|
V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5). V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
|
-
- HY-B0590A
-
-
- HY-123986
-
|
CTPI-2
|
Mitochondrial Metabolism
|
Cancer
Inflammation/Immunology
|
|
CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a KD of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet. Antitumor activity.
|
-
- HY-B2070
-
-
- HY-107794
-
|
Clodronate disodium tetrahydrate
Disodium clodronate tetrahydrate
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl - competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain.
|
-
- HY-B0327A
-
-
- HY-B0327
-
-
- HY-B0962A
-
-
- HY-B0962
-
-
- HY-B0457
-
-
- HY-121879
-
-
- HY-N0480A
-
-
- HY-N0480
-
-
- HY-128723
-
-
- HY-N0322
-
|
Cholesterol
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Metabolic Disease
|
|
Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
|
-
- HY-17530
-
|
Aldicarb sulfone
|
AChE
|
Others
|
|
Aldicarb sulfone(Temik sulfone) is a carbamate insecticide; is a cholinesterase inhibitor which prevents the breakdown of acetylcholine in the synapse.
|
-
- HY-B0457AS
-
-
- HY-B0457S
-
-
- HY-10716A
-
|
PF-03463275
|
GlyT
|
Neurological Disease
|
|
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
|
-
- HY-133541
-
|
Glucopiericidin A
|
GLUT
ADC Cytotoxin
Apoptosis
|
Cancer
|
|
Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A (PA; HY-114936) and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts.
|
-
- HY-U00067
-
-
- HY-B0882
-
|
Edrophonium chloride
|
AChE
|
Neurological Disease
|
|
Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
- HY-110176
-
|
ASP2535
|
GlyT
|
Neurological Disease
|
|
ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease.
|
-
- HY-17360
-
|
Tiotropium Bromide
BA679 BR
|
mAChR
|
Neurological Disease
|
|
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
|
-
- HY-19373
-
-
- HY-U00439A
-
|
Protein kinase inhibitors 1 hydrochloride
(E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride
|
DYRK
|
Cancer
|
|
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
|
-
- HY-13596
-
-
- HY-B0527A
-
-
- HY-B0106
-
-
- HY-B1547A
-
-
- HY-112843
-
|
CNT2 inhibitor-1
|
Others
|
Others
|
|
CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
|
-
- HY-B0827
-
|
Dinotefuran
MTI-446
|
Parasite
nAChR
|
Infection
|
|
Dinotefuran is an insecticide of the neonicotinoid class, its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors.
|
-
- HY-N7004
-
-
- HY-101334
-
|
MPDC
|
GlyT
|
Neurological Disease
|
|
MPDC is a potent and competitive inhibitor of the Na+-dependent high-affinity glutamate transporter in forebrain synaptosomes.
|
-
- HY-10010
-
|
Ko 143
|
BCRP
|
Cancer
|
|
Ko 143 is a potent and selective ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor. Ko 143 displays >200-fold selectivity over P-gp and MRP-1 transporters.
|
-
- HY-114381
-
-
- HY-101036
-
|
Choline bitartrate
|
mAChR
|
Neurological Disease
|
|
Choline (bitartrate) is an essential nutrient, often associated with the B vitamins but not yet officially defined as a B vitamin. Choline (bitartrate) plays an important role in synthesis of the neurotransmitter acetylcholine.
|
-
- HY-10914
-
-
- HY-B0034
-
|
Donepezil Hydrochloride
E2020
|
AChE
|
Neurological Disease
|
|
Donepezil (Hydrochloride) (E-2020) is a noncompetitive acetylcholinesterase inhibitor, which can readily cross the blood brain barrier and increases the concentration of cortical acetylcholine.
|
-
- HY-B0942
-
-
- HY-W012037
-
|
8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
|
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
-
- HY-19411
-
|
SSR180711 hydrochloride
|
nAChR
|
Neurological Disease
|
|
SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus.
|
-
- HY-14261
-
-
- HY-124738
-
-
- HY-B0590S1
-
-
- HY-50730
-
|
Asparagusic acid
|
Parasite
|
Infection
|
|
Asparagusic acid a sulfur-containing flavor component produced by Asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- HY-B0489
-
-
- HY-U00316
-
-
- HY-16423
-
-
- HY-101743
-
-
- HY-115292
-
|
Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
|
|
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
|
-
- HY-100390
-
|
(S)-ML753286
|
BCRP
|
Cancer
|
|
(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
|
-
- HY-B1110
-
|
Nomifensine
(±)-Nomifensin
|
Dopamine Receptor
|
Neurological Disease
|
|
Nomifensine is a norepinephrine-dopamine reuptake inhibitor, increases the amount of synaptic norepinephrine and dopamine available to receptors by blocking the dopamine and norepinephrine reuptake transporters.
|
-
- HY-13248
-
-
- HY-14258
-
|
Escitalopram
(S)-Citalopram; (S)-(+)-Citalopram
|
Serotonin Transporter
|
Neurological Disease
|
|
Escitalopram ((S)-Citalopram), the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram is an antidepressant for the research of major depression.
|
-
- HY-19331
-
|
WZB117
|
GLUT
|
Cancer
|
|
WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.
|
-
- HY-101037
-
|
Sarcosine
N-Methylglycine; Sarcosin
|
Endogenous Metabolite
GlyT
|
Cancer
|
|
Sarcosine is a glycine transporter type 1 (GlyT) inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site.
|
-
- HY-12850A
-
-
- HY-107526
-
|
NFPS
|
GlyT
|
Neurological Disease
|
|
NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively. NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion.
|
-
- HY-B1490
-
-
- HY-135813
-
|
LtaS-IN-1
|
Bacterial
|
Infection
|
|
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
|
-
- HY-14258A
-
|
Escitalopram oxalate
(S)-Citalopram oxalate; (S)-(+)-Citalopram oxalate
|
Serotonin Transporter
|
Neurological Disease
|
|
Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression.
|
-
- HY-107522
-
|
DL-TBOA
|
EAAT2
|
Neurological Disease
|
|
DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.
|
-
- HY-15258A
-
|
Lesinurad sodium
RDEA-594 sodium
|
URAT1
|
Metabolic Disease
|
|
Lesinurad sodium is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.
|
-
- HY-15258
-
|
Lesinurad
RDEA594
|
URAT1
|
Metabolic Disease
|
|
Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.
|
-
- HY-B0602
-
|
Desvenlafaxine
O-Desmethylvenlafaxine
|
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
|
-
- HY-101918
-
|
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-N0443
-
|
N-Methylcytisine
Caulophylline
|
nAChR
|
Inflammation/Immunology
|
|
N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia.
|
-
- HY-N0749
-
|
Jatrorrhizine
|
AChE
5-HT Receptor
Bacterial
|
Neurological Disease
|
|
Jatrorrhizine is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
|
-
- HY-B0602A
-
|
Desvenlafaxine succinate hydrate
O-Desmethylvenlafaxine succinate hydrate
|
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine succinate hydrate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate hydrate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
|
-
- HY-N0740
-
|
Jatrorrhizine chloride
|
AChE
5-HT Receptor
Bacterial
|
Inflammation/Immunology
Neurological Disease
|
|
Jatrorrhizine chloride is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine chloride is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine chloride reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
|
-
- HY-100152
-
-
- HY-B1205A
-
-
- HY-16787
-
|
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-N0749A
-
|
Jatrorrhizine hydroxide
|
AChE
5-HT Receptor
Bacterial
|
Inflammation/Immunology
Neurological Disease
|
|
Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
|
-
- HY-N2368
-
|
Arecaidine
|
GABA Receptor
|
Neurological Disease
|
|
Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H +-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
|
-
- HY-125957
-
|
A-3 hydrochloride
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
|
-
- HY-18974
-
-
- HY-15430A
-
-
- HY-14774
-
|
Monepantel
AAD1566
|
nAChR
|
Cancer
|
|
Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
|
-
- HY-B0726
-
-
- HY-N2332A
-
-
- HY-B0429
-
|
Pancuronium dibromide
|
nAChR
|
Neurological Disease
|
|
Pancuronium dibromide, a bis-quaternary steroid, is a neuromuscular relaxant. Pancuronium dibromide inhibits neuromuscular transmission by competing with acetylcholine for binding sites on nACh receptors. Pancuronium dibromide also inhibits cardiac muscarinic receptors and has a sympathomimetic action.
|
-
- HY-19264
-
|
264W94
|
Others
|
Metabolic Disease
|
|
264W94 is a potent ileal bile acid transporter (IBAT) inhibitor and a new cholesterol lowering agent. 264W94 has CYP7A1 induction, and antilipemic action.
|
-
- HY-100809
-
|
Guvacine hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
|
-
- HY-B1006
-
-
- HY-N1064
-
|
Xanthoplanine
|
nAChR
|
Neurological Disease
|
|
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
|
-
- HY-13217
-
|
Vanoxerine dihydrochloride
GBR-12909 dihydrochloride; I893 dihydrochloride
|
Dopamine Transporter
|
Neurological Disease
|
|
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT).
|
-
- HY-13217A
-
|
Vanoxerine
GBR 12909; I893
|
Dopamine Transporter
|
Neurological Disease
|
|
Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine (GBR-12909) binds to the target site on the dopamine transporter (DAT).
|
-
- HY-136450
-
|
Triclabendazole sulfoxide
TCBZ-SO
|
Parasite
BCRP
|
Infection
|
|
Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP.
|
-
- HY-128380
-
|
Dibenamine hydrochloride
N-(2-Chloroethyl)dibenzylamine hydrochloride
|
Adrenergic Receptor
|
Metabolic Disease
|
|
Dibenamine hydrochloride is a competitive and irreversible adrenergic blocking agent and is known to modify the pharmacological effects of epinephrine. Dibenamine hydrochloride cause a significant increase in the rate of destruction of I-epinephrine in the mouse.
|
-
- HY-107675
-
-
- HY-B0394
-
-
- HY-N3610
-
|
Coclaurine
|
nAChR
|
Neurological Disease
|
|
Coclaurine is a class of tetrahydroisoquinoline alkaloids isolated from Sarcopetalum harveyanum. Coclaurine is a nicotinic acetylcholine receptor (nAChRs) antagonist.
|
-
- HY-B0486
-
|
Lonidamine
AF-1890; Diclondazolic Acid; DICA
|
Hexokinase
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
Lonidamine (AF-1890), an antitumor agent, is a hexokinase, mitochondrial pyruvate carrier (Ki 2.5 μM in isolated rat liver mitochondria) and plasma membrane monocarboxylate transporters inhibitor, which also inhibits mitochondrial complex II.
|
-
- HY-15583
-
-
- HY-15790
-
|
Elobixibat
A 3309; AZD 7806
|
Others
|
Metabolic Disease
|
|
Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ± 0.17 nM, 0.13 ± 0.03 nM, and 5.8 ± 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
|
-
- HY-16191
-
|
ELR510444
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
|
-
- HY-15529
-
|
S0859
|
Na+/HCO3- Cotransporter
|
Cardiovascular Disease
|
|
S0859 is a selective, high-affinity generic Na +/HCO3 - transporter (NBC) inhibitor. S0859 reversibly inhibits NBC-mediated intracellular pH (pHi) recovery (Ki=1.7 μM, full inhibition at approximately 30 μM).
|
-
- HY-12157
-
|
VU 0238429
|
mAChR
|
Others
|
|
VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
|
-
- HY-15793
-
-
- HY-122470
-
|
Stampidine
|
Reverse Transcriptase
HIV
|
Infection
|
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
|
-
- HY-B1700A
-
|
Mivacurium dichloride
|
nAChR
|
Neurological Disease
|
|
Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell.
|
-
- HY-124658
-
|
G0507
|
Bacterial
|
Infection
|
|
G0507, a pyrrolopyrimidinedione compound, is a potent LolCDE ABC Transporter inhibitor. G0507 is a inhibitor of Escherichia coli growth and induces the extracytoplasmic σE stress response. G0507 acts as a chemical probe to dissect lipoprotein trafficking in Gram-negative bacteria.
|
-
- HY-B0823
-
|
Acetamiprid
|
nAChR
|
Neurological Disease
|
|
Acetamiprid is a neonicotinoid insecticide used worldwide. Acetamiprid is a nicotinic acetylcholine receptor (nAChR) agonist, and is shown to be associated with neuromuscular and reproductive disorders.
|
-
- HY-N0647
-
|
Silychristin
|
Others
|
Endocrinology
|
|
Silychristin is an abundant flavonolignan present in the fruits of Silybum marianum, with antioxidant properties. Silychristin is a potent inhibitor of the thyroid hormone transporter MCT8, and elicits a strong inhibition of T3 uptake with an IC50 of 110 nM.
|
-
- HY-108540
-
|
LAT1-IN-1
BCH
|
Apoptosis
|
Cancer
|
|
LAT1-IN-1 (BCH) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis.
|
-
- HY-B0520A
-
|
Benztropine mesylate
Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate
|
Dopamine Receptor
mAChR
Histamine Receptor
|
Cancer
Neurological Disease
|
|
Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
|
-
- HY-12741
-
|
LDN-212320
LDN-0212320; OSU-0212320
|
EAAT2
|
Neurological Disease
|
|
LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC[1]
|
-
- HY-B0106A
-
-
- HY-124540B
-
-
- HY-N2003
-
|
D-Tetrahydropalmatine
|
Dopamine Receptor
|
Metabolic Disease
|
|
D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis. D-Tetrahydropalmatine is a Dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors. D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor.
|
-
- HY-B0937
-
|
Amprolium
|
Parasite
|
Infection
|
|
Amprolium is a coccidiostat used in poultry, is a thiamine analogue and blocks the thiamine transporter of Eimeria species by blocking thiamine uptake it prevents carbohydrate synthesis.
|
-
- HY-B0937A
-
|
Amprolium hydrochloride
|
Parasite
|
Infection
|
|
Amprolium hydrochloride is a coccidiostat used in poultry, is a thiamine analogue and blocks the thiamine transporter of Eimeria species by blocking thiamine uptake it prevents carbohydrate synthesis.
|
-
- HY-11007
-
|
GNF-2
|
Bcr-Abl
SARS-CoV
|
Cancer
|
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
|
-
- HY-N6608
-
|
Physostigmine
Eserine
|
AChE
|
Neurological Disease
|
|
Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and elevate acetylcholine levels in the brain. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning.
|
-
- HY-14824
-
|
Sofiniclin
ABT 894
|
nAChR
|
Neurological Disease
|
|
Sofiniclin (ABT 894), an agonist of nicotinic acetylcholine receptor (nAChR), is used as a potential non-stimulant research for attention-deficit/hyperactivity disorder (ADHD).
|
-
- HY-W008610
-
|
GBR 12783
|
Dopamine Receptor
|
Neurological Disease
|
|
GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats.
|
-
- HY-100968
-
|
GBR 12783 dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats.
|
-
- HY-W008719
-
|
MPP+ iodide
|
Mitochondrial Metabolism
|
Neurological Disease
|
|
MPP+ iodide, a toxic metabolite of the neurotoxin MPTP, causes symptom of Parkinson's disease in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ iodide is taken up by the dopamine transporter into dopaminergic neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain. MPP+ iodide is also a high affinity substrate for the serotonin transporter (SERT).
|
-
- HY-D0067
-
|
7ACC1
DEAC; Coumarin D 1421; D 1421
|
Monocarboxylate Transporter
|
Cancer
|
|
7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
|
-
- HY-19753
-
|
KS176
|
BCRP
|
Cancer
|
|
KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively). Displays no inhibitory activity against P-gp or MRP1.
|
-
- HY-114395
-
|
NVS-ZP7-4
|
Others
|
Inflammation/Immunology
|
|
NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
|
-
- HY-N6936
-
|
Sennidin A
|
HCV
Akt
GLUT
|
Infection
|
|
Sennidin A, isolated from the leaves of Cassia angustifolia, inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation.
|
-
- HY-N7421
-
|
Smilagenin acetate
|
Others
|
Neurological Disease
|
|
Smilagenin acetate is a Sapogenin derivative extracted from patent US20030004147A1. Smilagenin acetate increases the expression of acetylcholine m2 receptors and can be used for the research of dementia.
|
-
- HY-111928
-
-
- HY-B1793
-
-
- HY-100228A
-
-
- HY-N2338
-
-
- HY-17604
-
|
Bexagliflozin
EGT1442; EGT0001442; THR-1442
|
SGLT
|
Metabolic Disease
|
|
Bexagliflozin (EGT1442) is a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor, with IC50s of 2 nM and 5.6 μM for human SGLT2 and SGLT1, respectively. Bexagliflozin can be used for the research of type 2 diabetic.
|
-
- HY-B0590B
-
|
(+)-Tetrabenazine
(+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine
|
Monoamine Transporter
|
Cancer
|
|
(+)-Tetrabenazine ((+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2), inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1.
|
-
- HY-101849
-
|
Fasentin
|
GLUT
|
Cancer
Cardiovascular Disease
|
|
Fasentin, a potent glucose transport inhibitor, inhibits GLUT-1 and GLUT-4 transporters. Fasentin is a chemical sensitizer to the death receptor stimuli FAS and tumor necrosis factor (TNF) apoptosis-inducing ligand. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity.
|
-
- HY-101453
-
|
Ceefourin 1
|
Others
|
Cancer
|
|
Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma.
|
-
- HY-101381
-
|
Otenzepad
AF-DX 116
|
mAChR
|
Metabolic Disease
Neurological Disease
|
|
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively.
|
-
- HY-W013093
-
-
- HY-122312
-
|
BAY-8002
|
Monocarboxylate Transporter
|
Cancer
|
|
BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity.
|
-
- HY-B0820
-
|
Nitenpyram
|
nAChR
|
Neurological Disease
|
|
Nitenpyram is a calss of neonicotinoid and an insect nicotinic acetylcholine receptor (nAChR) agonist with an IC50 of 14 nM. Nitenpyram is an oral fast-acting insecticide used to suppress sucking insects on companion animals.
|
-
- HY-12149
-
|
A-867744
|
nAChR
Autophagy
|
Neurological Disease
|
|
A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.
|
-
- HY-B1396
-
-
- HY-B1205
-
|
Atropine
Tropine tropate; DL-Hyoscyamine
|
mAChR
Endogenous Metabolite
|
Neurological Disease
|
|
Atropine (Tropine tropate) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist, with anti-myopia effect. Atropine blocks the inhibitory effect of ACh on heart rate and contractility, potentially also leading to tachyarrhythmias.
|
-
- HY-100806
-
-
- HY-107512
-
-
- HY-12560D
-
-
- HY-111678
-
|
ML230
CID44640177; SID 88095709
|
BCRP
|
Cancer
|
|
ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC50s values of 0.13 μM and 4.65 μM, respectively.
|
-
- HY-126301
-
-
- HY-107372
-
-
- HY-110241
-
|
Dianicline dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of drugs that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner.
|
-
- HY-120139
-
|
KMH-233
|
Others
|
Cancer
|
|
KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM).
|
-
- HY-125176
-
|
G907
|
Bacterial
|
Infection
|
|
G907 is a selective small-molecule antagonist of ATP-binding cassette (ABC) transporter, MsbA. It inhibits purified E. coli MsbA in amphipols with an IC50 of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket. Bactericidal activity.
|
-
- HY-107625A
-
|
SNAP 94847 hydrochloride
|
MCHR1 (GPR24)
|
Neurological Disease
|
|
SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
|
-
- HY-16643
-
|
Linerixibat
GSK2330672
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
|
Linerixibat (GSK2330672) is a highly potent, nonabsorbable and orally active apical sodium-dependent bile acid transporter (ASBT) inhibitor with an IC50 of 42 nM human ASBT. Linerixibat can be used as lipid-lowering agent. Linerixibat has the potential for type 2 diabetes and Primary Biliary Cholangitis treatment.
|
-
- HY-N6935
-
|
Sennidin B
|
HCV
Akt
GLUT
|
Infection
Metabolic Disease
|
|
Sennidin B, a stereoisomer isolated from the leaves of Cassia angustifolia, has lower activity than Sennidin A. Sennidin A inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation .
|
-
- HY-N7247
-
|
Thiochrome
|
mAChR
|
Metabolic Disease
|
|
Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors.
|
-
- HY-117203A
-
|
CDK12-IN-E9
|
CDK
|
Cancer
|
|
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.
|
-
- HY-N0801
-
|
Polygalacic acid
|
MMP
AChE
|
Inflammation/Immunology
Neurological Disease
|
|
Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment .
Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex.
|
-
- HY-122190
-
|
TAK-071
|
mAChR
|
Neurological Disease
|
|
TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.
|
-
- HY-112209
-
|
VU0467154
|
mAChR
|
Neurological Disease
|
|
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
|
-
- HY-101281A
-
|
(Rac)-VU 6008667
|
mAChR
|
Neurological Disease
|
|
(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
|
-
- HY-125901
-
|
D-Tubocurarine chloride pentahydrate
|
nAChR
|
Neurological Disease
|
|
D-Tubocurarine chloride pentahydrate is the chloride salt form of Tubocurarine, a nicotinic acetylcholine receptors (AChR) antagonist, and can be used as a skeletal muscle relaxant during surgery or mechanical ventilation. D-Tubocurarine chloride pentahydrate is also a potent neuromuscular blocking agent.
|
-
- HY-P1269
-
|
α-Conotoxin AuIB
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin AuIB, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.
|
-
- HY-114395A
-
|
(R)-NVS-ZP7-4
|
Others
|
Inflammation/Immunology
|
|
(R)-NVS-ZP7-4 is the R-isomer of NVS-ZP7-4. NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
|
-
- HY-B1190A
-
|
Cefadroxil hydrate
BL-S 578 hydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Cefadroxil hydrate (BL-S 578 hydrate) is an orally active and first-generation cephalosporin with a broad spectrum antibacterial activity. Cefadroxil hydrate (BL-S 578 hydrate) also acts as a substrate of the peptide transporter PEPT1 and PEPT2.
|
-
- HY-12560A
-
|
PNU-282987
|
nAChR
|
Neurological Disease
|
|
PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).
|
-
- HY-P1269A
-
-
- HY-15793A
-
|
Trans (2,3)-Dihydrotetrabenazine
(2R,3R,11bR)-rel-Dihydrotetrabenazine; (2R,3R,11bR)-rel-DHTBZ
|
Drug Metabolite
Monoamine Transporter
|
Neurological Disease
|
|
Trans (2,3)-Dihydrotetrabenazine ((2R,3R,11bR)-rel-Dihydrotetrabenazine), a metabolite of Tetrabenazine, shows remarkable inhibition activity on vesicular monoamine transporter (VMAT2).
|
-
- HY-14348
-
|
GSK163090
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities.
|
-
- HY-N0406
-
|
2"-O-beta-L-galactopyranosylorientin
|
Others
|
Metabolic Disease
|
|
2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2).
|
-
- HY-15084A
-
|
(-)-Dizocilpine maleate
(-)-MK-801 maleate
|
iGluR
|
Neurological Disease
|
|
(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects.
|
-
- HY-B2155
-
|
Acotiamide monohydrochloride trihydrate
|
AChE
|
Metabolic Disease
|
|
Acotiamide monohydrochloride trihydrate is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia. Acotiamide monohydrochloride trihydrate enhances acetylcholine released by enteric neurons through muscarinic receptor antagonism and acetylcholinesterase (AChE) inhibition, thereby enhancing gastric emptying and gastric accommodation.
|
-
- HY-P1268
-
|
α-Conotoxin PIA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
|
-
- HY-10936
-
|
S 18986
|
iGluR
|
Neurological Disease
|
|
S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
|
-
- HY-106901A
-
|
Asoxime dichloride
HI-6
|
nAChR
|
Neurological Disease
|
|
Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system.
|
-
- HY-W008344
-
|
2-Chloroadenosine
|
Others
|
Others
|
|
2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes.
|
-
- HY-N0173
-
|
Cinchonidine
α-Quinidine
|
Serotonin Transporter
Parasite
|
Infection
|
|
Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities.
|
-
- HY-P1268A
-
|
α-Conotoxin PIA TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PIA TFA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
|
-
- HY-100619
-
|
BMS-986020
|
LPL Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
BMS-986020 is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
|
-
- HY-100619A
-
|
BMS-986020 sodium
|
LPL Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
|
-
- HY-P1264
-
|
α-Bungarotoxin
|
nAChR
|
Neurological Disease
|
|
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM.
|
-
- HY-76772
-
|
Cevimeline hydrochloride hemihydrate
SNI-2011; AF102B hydrochloride hemihydrate
|
mAChR
|
Neurological Disease
|
|
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).
|
-
- HY-70020B
-
|
Cevimeline hydrochloride
AF102B hydrochloride
|
mAChR
|
Neurological Disease
|
|
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).
|
-
- HY-N4137
-
-
- HY-128974
-
|
N-Dodecyl-β-D-maltoside
Lauryl Maltoside
|
Others
|
Others
|
|
N-Dodecyl-β-D-maltoside (Lauryl Maltoside) is a derivatives of pyrene (Py), and it is a alkyl maltopyranoside detergent, especially in transporters and respiratory complexes. N-Dodecyl-β-D-maltoside has also been employed in applications such as in the purification and stabilization of RNA polymerase and detection of protein-lipid interactions.
|
-
- HY-12158
-
|
VU0238441
|
mAChR
|
Neurological Disease
|
|
VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively.
|
-
- HY-B1532
-
|
Anabasine
(S)-Anabasine; (+)-Anabasine
|
nAChR
|
Neurological Disease
|
|
Anabasine ((S)-Anabasine) is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC50=0.7 µM).
|
-
- HY-W014928
-
|
Anabasine hydrochloride
(S)-Anabasine hydrochloride; (+)-Anabasine hydrochloride
|
nAChR
|
Neurological Disease
|
|
Anabasine ((S)-Anabasine) hydrochloride is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC50=0.7 µM).
|
-
- HY-70020
-
|
Cevimeline
AF102B
|
mAChR
|
Neurological Disease
|
|
Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline can cross the blood-brain barrier (BBB).
|
-
- HY-12501A
-
|
ITI-214
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions.
|
-
- HY-13779
-
|
J-147
|
Monoamine Oxidase
Dopamine Transporter
|
Neurological Disease
|
|
J-147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. J-147 can readily pass the blood brain barrier (BBB). J-147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. J-147 has potential for the treatment of Alzheimer’s disease (AD).
|
-
- HY-134494
-
|
MS48107
|
Others
|
Neurological Disease
|
|
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice.
|
-
- HY-12501
-
|
ITI-214 free base
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.
|
-
- HY-107676
-
|
SIB-1553A
|
nAChR
|
Neurological Disease
|
|
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
|
-
- HY-10020
-
|
Varenicline Hydrochloride
CP 526555 hydrochloride
|
nAChR
|
Neurological Disease
|
|
Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a Ki value of 0.12 nM.
|
-
- HY-19838
-
|
JNJ-63533054
|
GPR139
|
Neurological Disease
|
|
JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB).
|
-
- HY-A0083
-
|
Methacholine chloride
Acetyl-β-methylcholine chloride
|
mAChR
|
Others
|
|
Methacholine (Acetyl-β-methylcholine) chloride acts a muscarinic M3 receptor agonist in the parasympathetic nervous system. Methacholine chloride acts directly on acetylcholine receptors on smooth muscle causing contraction and airway narrowing. Methacholine challenges are widely used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates.
|
-
- HY-100007
-
|
Vonoprazan
TAK-438 free base
|
Proton Pump
|
Endocrinology
|
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker, with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-N0755
-
|
Rhoifolin
|
Insulin Receptor
GLUT
NF-κB
p38 MAPK
Autophagy
|
Metabolic Disease
Endocrinology
Cancer
|
|
Rhoifolin is a flavone glycoside isolated from Citrus grandis (L.) Osbeck leaves. Rhoifolin is beneficial for diabetic complications through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways.
|
-
- HY-15310
-
|
Ivermectin
MK-933
|
Parasite
HIV
Mitophagy
HSV
SARS-CoV
Antibiotic
Autophagy
|
Infection
Cancer
|
|
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
|
-
- HY-P1365
-
|
α-Conotoxin MII
α-CTxMII
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII (α-CTxMII) potently blocks β3-containing neuronal nicotinic receptors .
|
-
- HY-10019
-
|
Varenicline
CP 526555
|
nAChR
|
Neurological Disease
|
|
Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment.
|
-
- HY-14564A
-
|
GTS-21 dihydrochloride
DMXB-A; DMBX-anabaseine
|
nAChR
5-HT Receptor
|
Inflammation/Immunology
|
|
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist .
|
-
- HY-P1365A
-
|
α-Conotoxin MII TFA
α-CTxMII TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin MII TFA (α-CTxMII TFA), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII TFA (α-CTxMII TFA) potently blocks β3-containing neuronal nicotinic receptors .
|
-
- HY-15697
-
|
TUG-770
|
GPR40
|
Metabolic Disease
|
|
TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research.
|
-
- HY-109067
-
|
Opiranserin
|
GlyT
5-HT Receptor
P2X Receptor
|
Neurological Disease
|
|
Opiranserin, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain.
|
-
- HY-136233
-
|
PSB 0777 ammonium
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research.
|
-
- HY-116594A
-
-
- HY-136207
-
|
TC-2559 difumarate
|
nAChR
|
Neurological Disease
|
|
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
|
-
- HY-116594
-
|
OPC-14523 free base
|
Sigma Receptor
5-HT Receptor
|
Neurological Disease
|
|
OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity.
|
-
- HY-14565
-
|
Pozanicline
ABT-089
|
nAChR
|
Neurological Disease
|
|
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM.
Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.
|
-
- HY-103430
-
|
SKF-83566 hydrobromide
|
Dopamine Receptor
5-HT Receptor
Adenylate Cyclase
|
Neurological Disease
|
|
SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation.
|
-
- HY-103430A
-
|
SKF-83566
|
Dopamine Receptor
5-HT Receptor
Adenylate Cyclase
|
Neurological Disease
|
|
SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation.
|
-
- HY-124619
-
|
GPI-1046
|
FKBP
HIV
|
Infection
Neurological Disease
|
|
GPI-1046 is a immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core. GPI-1046 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models. GPI-1046 readily crosses the blood-brain barrier and promotes the regeneration of dopamine (DA) cells in the CNS in association with functional recovery in rodent models. GPI-1046 improves HIV-associated injury of peripheral nerves.
|
-
- HY-137471
-
|
RBPJ Inhibitor-1
RIN1
|
Notch
|
Cancer
|
|
RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
|
-
- HY-136121
-
|
Tubulin inhibitor 6
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
|
-
- HY-112812
-
-
- HY-B0552A
-
-
- HY-112911
-
-
- HY-B0552
-
-
- HY-18353
-
|
mTOR inhibitor-3
|
mTOR
|
Cancer
|
|
mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
|
-
- HY-112722
-
-
- HY-137497
-
|
KRAS inhibitor-9
|
Ras
Apoptosis
|
Cancer
|
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
|
-
- HY-D0843
-
|
N-Ethylmaleimide
NEM
|
Cathepsin
Deubiquitinase
|
Others
|
|
N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.
|
-
- HY-101275
-
-
- HY-13278A
-
-
- HY-111412
-
-
- HY-21141
-
|
Cysteine protease inhibitor-2
|
Cathepsin
|
Cancer
|
|
Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
|
-
- HY-17541A
-
-
- HY-17541
-
-
- HY-112914
-
-
- HY-70005
-
-
- HY-128703
-
-
- HY-10442
-
-
- HY-12186
-
|
3-Deazaneplanocin A hydrochloride
DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.
|
-
- HY-128722
-
-
- HY-110101
-
-
- HY-12202
-
-
- HY-B0543
-
-
- HY-10421
-
-
- HY-B0385
-
-
- HY-P0017
-
-
- HY-32015
-
|
Cot inhibitor-1
|
MAP3K
|
Inflammation/Immunology
|
|
Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM.
|
-
- HY-136279
-
|
TrxR inhibitor D9
|
Apoptosis
|
Cancer
|
|
TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.
|
-
- HY-101297
-
|
Z-IETD-FMK
Z-IE(OMe)TD(OMe)-FMK
|
Caspase
|
Cancer
|
|
Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
|
-
- HY-100732
-
|
Cambinol
|
Sirtuin
Apoptosis
Phospholipase
|
Cancer
|
|
Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-15182
-
-
- HY-112474
-
-
- HY-136920
-
-
- HY-13662
-
-
- HY-13662A
-
-
- HY-119937
-
-
- HY-15253
-
-
- HY-13973A
-
-
- HY-104051
-
-
- HY-111347A
-
-
- HY-131100
-
-
- HY-135890
-
-
- HY-15444
-
-
- HY-112390A
-
|
Syk Inhibitor II
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
|
-
- HY-122723
-
|
GOT1 inhibitor-1
|
Others
|
Cancer
|
|
GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC).
|
-
- HY-114317
-
|
MARK4 inhibitor 1
|
Apoptosis
|
Cancer
|
|
MARK4 inhibitor 1 is a potent microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.
|
-
- HY-15002
-
|
AST 487
NVP-AST 487
|
RET
FLT3
VEGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
|
-
- HY-135826
-
|
Necroptosis-IN-1
|
RIP kinase
|
Cancer
|
|
Necroptosis-IN-1, an analog of Necrostatin-1 (HY-15760), is a potent necroptosi inhibitor. Necroptosis-IN-1 is a RIPK inhibitor.
|
-
- HY-111408
-
-
- HY-N2033
-
-
- HY-100463
-
-
- HY-112607
-
|
Tubulin inhibitor 1
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
|
-
- HY-124798
-
-
- HY-32018
-
|
Cot inhibitor-2
|
MAP3K
|
Cancer
|
|
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
|
-
- HY-B0884
-
-
- HY-112569
-
-
- HY-B0884A
-
-
- HY-15167
-
-
- HY-112906
-
-
- HY-50856A
-
-
- HY-117262
-
-
- HY-U00410
-
-
- HY-13276
-
-
- HY-B0218
-
-
- HY-106067A
-
-
- HY-N6717
-
|
Tentoxin
|
Others
|
Infection
|
|
Tentoxin is a cyclic tetrapeptide isolated from Alternaria tenuis, acts as a herbicide, causes seedling chlorosis, inhibits cyclic photophosphorylation and functions as an energy transfer inhibitor.
|
-
- HY-17542
-
|
PLpro inhibitor
|
SARS-CoV
|
Infection
|
|
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM.
|
-
- HY-15760
-
-
- HY-N1504
-
|
Loureirin B
|
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-13662B
-
|
(R)-Lansoprazole
Dexlansoprazole
|
Proton Pump
|
Inflammation/Immunology
|
|
(R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-10217
-
-
- HY-P1029
-
-
- HY-15604
-
-
- HY-N0565
-
-
- HY-15183
-
-
- HY-U00387
-
-
- HY-107986
-
-
- HY-10249A
-
-
- HY-100962
-
|
(E)-AG 99
(E)-Tyrphostin 46; (E)-Tyrphostin AG 99
|
EGFR
|
Cancer
|
|
(E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
|
-
- HY-N0565A
-
-
- HY-108322
-
-
- HY-50880
-
-
- HY-N2221
-
-
- HY-14657
-
-
- HY-101932
-
-
- HY-N6902
-
-
- HY-U00319
-
-
- HY-15825
-
|
IWP L6
Porcn Inhibitor III
|
Porcupine
|
Cancer
|
|
IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC50 of 0.5 nM.
|
-
- HY-112269
-
-
- HY-50879
-
-
- HY-104032
-
-
- HY-10172
-
|
IMD-0354
IKK2 Inhibitor V
|
IKK
|
Cancer
|
|
IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
|
-
- HY-136270
-
|
ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
|
ATR inhibitor 2 is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
|
-
- HY-103310
-
-
- HY-122856
-
|
AZ12601011
|
TGF-β Receptor
|
Cancer
|
|
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
|
-
- HY-50900
-
-
- HY-B0083
-
|
Leflunomide
HWA486; RS-34821; SU101
|
Others
|
Cancer
|
|
Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.
|
-
- HY-101474A
-
|
Zanubrutinib
BGB-3111
|
Btk
|
Cancer
|
|
Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.
|
-
- HY-16569
-
-
- HY-N7592
-
|
Arjunetin
|
Others
|
Others
|
|
Arjunetin, isolated from Terminalia arjuna, is an insect feeding-deterrent and growth inhibitor.
|
-
- HY-W008923
-
-
- HY-12238
-
|
IWR-1
endo-IWR 1; IWR-1-endo
|
Wnt
|
Cancer
|
|
IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
|
-
- HY-100110
-
|
KNK437
Heat Shock Protein Inhibitor I
|
HSP
|
Cancer
|
|
KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
|
-
- HY-135384
-
-
- HY-106638
-
-
- HY-100933
-
-
- HY-A0276
-
|
Gentamicin sulfate
|
Bacterial
Antibiotic
|
Infection
|
|
Gentamicin sulfate, an aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. It inhibits DNase I with an IC50 of 0.57 mM.
|
-
- HY-N0518
-
|
Toddalolactone
|
PAI-1
|
Cardiovascular Disease
|
|
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
|
-
- HY-16657
-
-
- HY-19931
-
|
COH29
RNR Inhibitor COH29
|
DNA/RNA Synthesis
|
Cancer
|
|
COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
|
-
- HY-119808
-
-
- HY-128729
-
|
DNA2 inhibitor C5
|
Others
|
Cancer
|
|
DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress.
|
-
- HY-P2478
-
-
- HY-13624A
-
|
Epirubicin hydrochloride
4'-Epidoxorubicin hydrochloride
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-P2477
-
-
- HY-15358
-
|
ALK inhibitor 2
|
ALK
FAK
|
Cancer
|
|
ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=37 nM) and focal adhesion kinase (FAK; IC50=5 nM).
|
-
- HY-10917
-
|
GW2580
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.
|
-
- HY-15357
-
|
ALK inhibitor 1
|
ALK
FAK
|
Cancer
|
|
ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
|
-
- HY-13624
-
|
Epirubicin
4'-Epidoxorubicin
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-13417A
-
|
AICAR phosphate
Acadesine phosphate; AICA Riboside phosphate
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-113951
-
-
- HY-124718
-
|
p32 Inhibitor M36
M36
|
PKC
|
Cancer
|
|
p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.
|
-
- HY-13417
-
|
AICAR
Acadesine; AICA Riboside
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-P1260
-
-
- HY-19797A
-
-
- HY-14274
-
|
Anastrozole
ZD1033
|
Aromatase
|
Cancer
|
|
Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
|
-
- HY-131101
-
|
Nor-Acetildenafil
|
Others
|
Others
|
|
Nor-Acetildenafil is an Acetildenafil derivative. Acetildenafil is a synthetic agent which acts as a phosphodiesterase inhibitor.
|
-
- HY-10846
-
-
- HY-18930
-
|
NU6300
|
CDK
|
Cancer
|
|
NU6300 is the first covalent, irreversible and ATP-competitive CDK2 inhibitor.
|
-
- HY-W013478
-
-
- HY-15700
-
-
- HY-101429
-
|
RG13022
Tyrphostin RG13022
|
EGFR
|
Cancer
|
|
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
|
-
- HY-B1877
-
|
Nitrofen
|
Others
|
Cancer
|
|
Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.
|
-
- HY-N2219
-
-
- HY-19795
-
|
ML240
|
p97
|
Cancer
|
|
ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC50 value of 100 nM.
|
-
- HY-112639
-
-
- HY-100600
-
|
BGG463
K03859
|
CDK
|
Others
|
|
BGG463 (K03859) is an orally active type II CDK2 inhibitor.
|
-
- HY-N2117
-
|
Isoginkgetin
|
MMP
|
Cancer
|
|
Isoginkgetin is a MMP-9 inhibitor, also a Pre-mRNA Splicing Inhibitor with IC 50 of 30 uM.
|
-
- HY-136461
-
-
- HY-P2564
-
-
- HY-15222
-
-
- HY-14196
-
-
- HY-17396
-
-
- HY-14440
-
|
MP7
PDK1 inhibitor
|
PDK-1
|
Cancer
|
|
MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
|
-
- HY-50670
-
-
- HY-U00145
-
-
- HY-B0113A
-
|
Omeprazole sodium
H 16868 sodium
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-12072
-
|
Lck Inhibitor
|
Src
|
Inflammation/Immunology
|
|
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
|
-
- HY-10255A
-
|
Sunitinib
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-111429
-
|
YAP/TAZ inhibitor-1
|
YAP
|
Cancer
|
|
YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor extracted from patent WO2017058716A1, Compound 1, has an IC50 of <0.100 μΜ in firefly luciferase assay.
|
-
- HY-120859
-
|
Zidebactam
WCK-5107
|
Bacterial
|
Infection
|
|
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-118355
-
|
ALLM
Calpain inhibitor II
|
Proteasome
Cathepsin
|
Neurological Disease
|
|
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).
|
-
- HY-12824
-
|
RNPA1000
|
Antibiotic
Bacterial
|
Infection
|
|
RNPA1000, an antibiotic, is a potent RnpA inhibitor and inhibits RnpA-mediated cellular RNA degradation. RNPA1000 inhibits tRNA maturation with an IC50 of 175 μM. RNPA1000 displays broad-spectrum antimicrobial activities and inhibits staphylococcal and all Gram-positive bacterial pathogens activity.
|
-
- HY-101019
-
|
Ossirene
AS101
|
Interleukin Related
Caspase
|
Cancer
Inflammation/Immunology
|
|
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.
|
-
- HY-100932
-
|
ML-9
|
Myosin
|
Cancer
|
|
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-B0113
-
|
Omeprazole
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-N0565B
-
|
Doxycycline (hyclate)
Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
|
MMP
Bacterial
Antibiotic
|
Infection
|
|
Doxycycline (hyclate) (Doxycycline hydrochloride hemiethanolate hemihydrate), an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
|
-
- HY-15699A
-
-
- HY-B2063
-
|
Chlorobenzuron
|
Others
|
Others
|
|
Chlorobenzuron is a chitin synthetase inhibitor, acts as an insecticide. Chlorobenzuron can inhibit larvae development and pupate.
|
-
- HY-N1447
-
-
- HY-15167A
-
-
- HY-112634
-
-
- HY-133248
-
-
- HY-13972
-
-
- HY-15699
-
-
- HY-118165
-
-
- HY-B1596
-
-
- HY-P1260A
-
-
- HY-103593A
-
-
- HY-15842
-
-
- HY-103593
-
|
LCL521
|
Phospholipase
|
Cancer
|
|
LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
|
-
- HY-I0637
-
-
- HY-16187
-
-
- HY-133247
-
-
- HY-D0886
-
-
- HY-18965
-
-
- HY-12277
-
|
AZ191
|
DYRK
|
Cancer
|
|
AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM.
|
-
- HY-107451
-
-
- HY-107485
-
-
- HY-14174
-
-
- HY-N7511
-
-
- HY-N4294
-
-
- HY-B2007
-
-
- HY-13818
-
-
- HY-100498
-
|
GSK2256098
|
FAK
Apoptosis
|
Cancer
|
|
GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
|
-
- HY-14445
-
-
- HY-19707
-
-
- HY-112822
-
|
ON-013100
|
CDK
|
Cancer
|
|
ON-013100, an antineoplastic drug, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.
|
-
- HY-100456
-
-
- HY-111493
-
-
- HY-50706A
-
|
Selumetinib sulfate
AZD6244 sulfate; ARRY-142886 sulfate
|
MEK
Apoptosis
|
Cancer
|
|
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-105917
-
|
Endovion
NS3728
|
Chloride Channel
|
Others
|
|
Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
|
-
- HY-10326
-
|
GW788388
|
TGF-β Receptor
|
Cancer
|
|
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
|
-
- HY-13228
-
-
- HY-126288
-
|
ERK1/2 inhibitor 2
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.
|
-
- HY-10227
-
|
Bortezomib
PS-341; LDP-341; NSC 681239
|
Proteasome
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
|
-
- HY-10255
-
|
Sunitinib Malate
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-17367
-
|
Atazanavir
BMS-232632
|
HIV
HIV Protease
Cytochrome P450
P-glycoprotein
|
Infection
Cancer
|
|
Atazanavir (BMS-232632) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
|
-
- HY-13985
-
-
- HY-12031A
-
-
- HY-U00453
-
-
- HY-112910
-
|
Grp94 Inhibitor-1
|
HSP
|
Cancer
Infection
|
|
Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.
|
-
- HY-15339
-
|
CVT-313
Cdk2 Inhibitor III
|
CDK
|
Cancer
|
|
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.
|
-
- HY-13984
-
|
Mutant EGFR inhibitor
|
EGFR
|
Cancer
|
|
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M.
|
-
- HY-22166
-
-
- HY-W047428
-
-
- HY-112451
-
-
- HY-15217
-
-
- HY-15859
-
|
Atglistatin
|
ATGL
|
Metabolic Disease
|
|
Atglistatin is a selective adipose triglyceride lipase (ATGL) inhibitor which inhibits lipolysis with an IC50 of 0.7 μM in vitro.
|
-
- HY-77521
-
-
- HY-13502
-
-
- HY-107994
-
-
- HY-70027A
-
-
- HY-N2567
-
|
(±)-Decursinol
|
Bacterial
|
Cancer
|
|
(±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC50 of 102 μM.
|
-
- HY-13278
-
-
- HY-112860
-
-
- HY-12000
-
-
- HY-A0116S
-
-
- HY-13060
-
-
- HY-101474
-
|
(±)-Zanubrutinib
(±)-BGB-3111
|
Btk
|
Cancer
|
|
(±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
|
-
- HY-19731
-
-
- HY-101462
-
-
- HY-B0902A
-
|
Rufloxacin hydrochloride
MF-934 hydrochloride
|
Bacterial
|
Infection
|
|
Rufloxacin hydrochloride (MF-934 hydrochloride) is a fluoroquinolone antibacterial, inhibits B-cell differentiation in human mononuclear cells, inhibits Topo.
|
-
- HY-101963
-
-
- HY-70073
-
-
- HY-15775
-
-
- HY-13502A
-
-
- HY-70003
-
-
- HY-112720
-
-
- HY-111784
-
-
- HY-10439
-
|
HPGDS inhibitor 1
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
|
-
- HY-100816
-
|
Rbin-1
Ribozinoindole-1
|
Phosphatase
|
Metabolic Disease
|
|
Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).
|
-
- HY-120675
-
|
SSTC3
|
Casein Kinase
Wnt
|
Cancer
|
|
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
|
-
- HY-100556
-
|
Tie2 kinase inhibitor 1
|
Others
|
Cancer
|
|
Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.
|
-
- HY-112715
-
-
- HY-14165
-
-
- HY-128918
-
|
SIS17
|
HDAC
|
Others
|
|
SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
|
-
- HY-124793
-
|
GAK inhibitor 49
|
Others
|
Infection
|
|
GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2.
|
-
- HY-P1111
-
|
Lyn peptide inhibitor
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-100932A
-
|
ML-9 Free Base
|
Myosin
|
Cancer
|
|
ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-135318
-
|
NBDHEX
|
Glutathione Peroxidase
Apoptosis
Autophagy
|
Cancer
|
|
NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
|
-
- HY-121172
-
|
1,4-DPCA
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM.
|
-
- HY-N0822
-
|
Shikonin
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
|
Cancer
|
|
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
|
-
- HY-12364
-
-
- HY-P0081
-
-
- HY-133110
-
|
Afatinib N-Oxide
|
Others
|
Others
|
|
Afatinib N-Oxide is a impurity of Afatinib dimaleate in oxidative degradation. Afatinib dimaleate is an irreversible EGFR family inhibitor.
|
-
- HY-15798
-
-
- HY-114418
-
-
- HY-N5038
-
|
Mauritianin
|
Topoisomerase
|
Cancer
|
|
Mauritianin is a kaempferol glycoside isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor.
|
-
- HY-13606
-
|
Dacinostat
NVP-LAQ824; LAQ824
|
HDAC
Autophagy
|
Cancer
|
|
Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.
|
-
- HY-13256
-
-
- HY-P1452A
-
-
- HY-Y0882
-
-
- HY-16420
-
|
R112
|
Syk
|
Inflammation/Immunology
|
|
R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM.
|
-
- HY-111919
-
-
- HY-15588
-
-
- HY-B0830
-
|
Isoprocarb
|
AChE
|
Neurological Disease
|
|
Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor.
|
-
- HY-N1502
-
|
Carboxyatractyloside
Gummiferin
|
Others
|
Cancer
|
|
Carboxyatractyloside is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport.
|
-
- HY-12054A
-
-
- HY-114423
-
-
- HY-10809
-
|
Bitopertin
RG1678; RO4917838
|
GlyT
|
Neurological Disease
|
|
Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
|
-
- HY-19609
-
-
- HY-131268
-
-
- HY-N6619A
-
|
Lycoramine
|
AChE
|
Neurological Disease
|
|
Lycoramine, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine is a potent acetylcholinesterase (AChE) inhibitor.
|
-
- HY-104028
-
-
- HY-12814
-
|
TH588
|
DNA/RNA Synthesis
|
Cancer
|
|
TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
|
-
- HY-12054
-
-
- HY-12420
-
|
JNJ-47117096 hydrochloride
MELK-T1 hydrochloride
|
MELK
FLT3
|
Cancer
|
|
JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM.
|
-
- HY-16982
-
|
Cercosporamide
(-)-Cercosporamide
|
Fungal
MNK
|
Cancer
Infection
|
|
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
|
-
- HY-136347
-
-
- HY-13280
-
-
- HY-N4186
-
-
- HY-103002
-
|
SU5408
VEGFR2 Kinase Inhibitor I
|
VEGFR
|
Cardiovascular Disease
|
|
SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
|
-
- HY-B0497B
-
-
- HY-131446
-
|
Chk1-IN-5
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.
|
-
- HY-50202
-
|
Etomoxir
(R)-(+)-Etomoxir
|
Apoptosis
|
Cancer
Metabolic Disease
|
|
Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-19727A
-
-
- HY-50202A
-
|
Etomoxir sodium salt
(R)-(+)-Etomoxir sodium salt
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-124416
-
|
ML604086
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca 2+ concentrations.
|
-
- HY-103490
-
|
Takinib
|
MAP3K
Apoptosis
|
Cancer
|
|
Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, which inhibits autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation.
|
-
- HY-17367A
-
|
Atazanavir sulfate
BMS-232632 sulfate
|
HIV
HIV Protease
Cytochrome P450
P-glycoprotein
|
Cancer
Infection
|
|
Atazanavir sulfate (BMS-232632 sulfate) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate (BMS-232632 sulfate) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
|
-
- HY-122866
-
|
ZT-12-037-01
|
Ras
|
Cancer
|
|
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM.
|
-
- HY-100227
-
|
E 64c
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
|
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-66004
-
|
4-Acetamidophenyl acetate
|
Others
|
Inflammation/Immunology
|
|
4-Acetamidophenyl acetate is an impurity of Acetaminophen (paracetamol). Acetaminophen, an analgesic drug, is a selective COX-2 inhibitor (IC50=25.8 μM), and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
|
-
- HY-115502
-
|
BCI
(E)-BCI
|
Phosphatase
|
Cancer
Inflammation/Immunology
|
|
BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5.
|
-
- HY-80003
-
|
QL47
|
Btk
|
Cancer
Infection
|
|
QL47, a broad-spectrum antiviral agent, inhibits dengue virus and other RNA viruses. QL47 selectively inhibits eukaryotic translation. QL47 is a potent covalent inhibitor of BTK with an IC50 of 7 nM.
|
-
- HY-15766A
-
|
GNE-617 hydrochloride
|
Nampt
|
Cancer
|
|
GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- HY-12399
-
|
MKC9989
|
IRE1
|
Cancer
|
|
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
|
-
- HY-101053
-
|
Src Inhibitor 1
Src Kinase Inhibitor 1; Src-l1
|
Src
|
Cancer
|
|
Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
|
-
- HY-10247
-
|
BRAF inhibitor
|
Raf
|
Cancer
|
|
BRAF inhibitor is a B-Raf inhibitor extracted from patent WO/2011103196 A1, Compound P-0850.
|
-
- HY-N2522
-
-
- HY-109565
-
|
ASTX660
|
IAP
|
Cancer
|
|
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
|
-
- HY-108820
-
-
- HY-108817
-
-
- HY-10978
-
-
- HY-13452
-
-
- HY-119459
-
|
Fluopyram
|
Fungal
|
Infection
|
|
Fluopyram is a succinate dehydrogenase inhibitor fungicide, inhibits the growth of F. virguliforme isolates with mean EC50 of 3.35 µg/mL.
|
-
- HY-135383A
-
-
- HY-A0122
-
-
- HY-17381
-
-
- HY-N6031
-
|
Dendrophenol
|
NF-κB
|
Cancer
|
|
Dendrophenol, isolated from the stem of Dendrobium loddigesii Rolfe, act as a NF-κB inhibitor. Antineoplastic activity.
|
-
- HY-Y0172
-
-
- HY-108941
-
|
Salicyl-AMS
|
Bacterial
|
Infection
|
|
Salicyl-AMS is a mycobactin biosynthesis inhibitor which can also inhibit M. tuberculosis growth in vitro under iron-limited conditions.
|
-
- HY-15282
-
-
- HY-B0806
-
|
Proguanil
|
Parasite
Antifolate
|
Infection
|
|
Proguanil, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
|
-
- HY-N2597
-
-
- HY-B0806A
-
-
- HY-13420
-
-
- HY-100736
-
|
ML348
GNF-Pf-1127
|
Phospholipase
|
Cancer
|
|
ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor with an IC50 of 210 nM, and barely inhibits LYPLA2.
|
-
- HY-15202
-
|
Binimetinib
MEK162; ARRY-162; ARRY-438162
|
MEK
Autophagy
|
Cancer
|
|
Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
|
-
- HY-12726
-
-
- HY-N1724
-
-
- HY-15766
-
|
GNE-617
|
Nampt
|
Metabolic Disease
Cancer
|
|
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- HY-111489B
-
-
- HY-126253
-
|
BI-4916
|
Others
|
Cancer
|
|
BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD +-competitive PHGDH inhibitor.
|
-
- HY-136485
-
-
- HY-B1863
-
|
Iprobenfos
|
Fungal
|
Infection
|
|
Iprobenfos is an organophosphorus fungicide and is widely used to control the rice blast fungus. Iprobenfos is also a choline biosynthesis inhibitor.
|
-
- HY-P1045
-
|
187-1, N-WASP inhibitor
|
Arp2/3 Complex
|
Others
|
|
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-124653
-
|
HSP27 inhibitor J2
J2
|
HSP
|
Cancer
|
|
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.
|
-
- HY-P1045A
-
|
187-1, N-WASP inhibitor TFA
|
Arp2/3 Complex
|
Others
|
|
187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-P1111A
-
|
Lyn peptide inhibitor TFA
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-135899
-
|
SIRT7 inhibitor 97491
|
Sirtuin
Apoptosis
|
Cancer
|
|
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..
|
-
- HY-B2145
-
|
Ilaprazole sodium
IY-81149 sodium
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-107412
-
|
Proteasome inhibitor IX
PS-IX; AM114
|
Proteasome
|
Cancer
|
|
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 +/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity.
|
-
- HY-130795
-
|
GSK-3β inhibitor 2
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
|
-
- HY-100899
-
-
- HY-101705
-
-
- HY-N7674A
-
|
Angoline hydrochloride
|
STAT
|
Cancer
|
|
Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
|
-
- HY-P1290
-
|
PKA Inhibitor Fragment (6-22) amide
PKI-(6-22)-amide
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-10009
-
-
- HY-N7674
-
|
Angoline
|
STAT
|
Cancer
|
|
Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
|
-
- HY-100734
-
-
- HY-123772
-
|
CDK5 inhibitor 20-223
|
CDK
|
Cancer
|
|
CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.
|
-
- HY-N6619
-
-
- HY-109877
-
-
- HY-100299
-
-
- HY-P2470
-
-
- HY-50710
-
|
KU-0063794
|
mTOR
|
Cancer
|
|
KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC50s of 10 nM.
|
-
- HY-137239
-
-
- HY-100303A
-
|
FR194738
|
Others
|
Metabolic Disease
|
|
FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
|
-
- HY-50946
-
-
- HY-15886
-
-
- HY-112131
-
-
- HY-19326
-
-
- HY-12971
-
|
Nampt-IN-1
LSN3154567
|
Nampt
|
Cancer
|
|
Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.
|
-
- HY-101479
-
|
Iclaprim
AR-100
|
Bacterial
|
Infection
|
|
Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.
|
-
- HY-70027
-
-
- HY-108900A
-
-
- HY-N5118
-
|
Chimonanthine
(-)-Chimonanthine
|
Tyrosinase
|
Cancer
|
|
Chimonanthine is an alkaloid of Chimonanthus praecox, inhibits tyrosinase and tyrosine-related protein-1 mRNA expression, amd inhibits melanogenesis.
|
-
- HY-U00049
-
-
- HY-16904
-
|
RI-2
|
RAD51
|
Cancer
|
|
RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
|
-
- HY-130760
-
-
- HY-103036
-
-
- HY-111410
-
-
- HY-13229
-
|
BOC-D-FMK
|
Caspase
|
Cancer
|
|
Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
|
-
- HY-10862
-
|
FAAH inhibitor 1
Benzothiazole analog 3
|
FAAH
Autophagy
|
Cancer
|
|
FAAH inhibitor 1 (Benzothiazole analog 3) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 18±8 nM.
|
-
- HY-13256A
-
|
Desmethyl Erlotinib
OSI-420 free base; CP-373420
|
Drug Metabolite
|
Cancer
|
|
Desmethyl Erlotinib (OSI-420 free base) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor.
|
-
- HY-15735
-
|
c-Met inhibitor 1
|
c-Met/HGFR
|
Cancer
|
|
c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer.
|
-
- HY-10997S
-
|
Ibrutinib D5
PCI-32765 D5
|
Btk
|
Cancer
|
|
Ibrutinib D5 (PCI-32765 D5) is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor.
|
-
- HY-15586
-
|
L67
DNA Ligase Inhibitor
|
DNA/RNA Synthesis
|
Cancer
|
|
L67 is a novel, competitive human DNA ligase inhibitor, inhibits DNA ligases I and III with IC50 of 10 μM and 10 μM.
|
-
- HY-B0008
-
-
- HY-115502A
-
|
BCI hydrochloride
(E)-BCI hydrochloride
|
Phosphatase
|
Cancer
Inflammation/Immunology
|
|
BCI hydrochloride ((E)-BCI hydrochloride) is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI hydrochloride specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI hydrochloride does not inhibit DUSP5.
|
-
- HY-12031
-
-
- HY-136538
-
|
LQZ-7I
|
Survivin
|
Cancer
|
|
LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors.
|
-
- HY-19727
-
-
- HY-N2006
-
|
Ganoderic acid B
|
HIV Protease
|
Infection
|
|
Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease.
|
-
- HY-P1376
-
|
G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
|
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-114169
-
|
WRG-28
|
Discoidin Domain Receptor
|
Cancer
|
|
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor with an IC50 of 230 nM. WRG-28 uniquely inhibits receptor-ligand interactions via allosteric modulation of the receptor. WRG-28 inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs by targeting DDR2.
|
-
- HY-16592
-
|
Brefeldin A
BFA; Cyanein; Decumbin
|
Autophagy
CRISPR/Cas9
Mitophagy
HSV
Antibiotic
|
Cancer
Infection
|
|
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
|
-
- HY-101664
-
|
Ilaprazole
IY-81149
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-112373
-
|
Aurora Kinase Inhibitor 3
|
Aurora Kinase
|
Others
|
|
Aurora Kinase Inhibitor 3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50>10 μM. Aurora Kinase Inhibitor 3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket, and several induced structural changes in the active-site compared with other published AIK structures.
|
-
- HY-135396
-
|
(1S,2S)-Bortezomib
|
Proteasome
|
Cancer
|
|
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
|
-
- HY-136149A
-
|
Mpro inhibitor N3 hemihydrate
|
SARS-CoV
Virus Protease
|
Infection
|
|
Mpro inhibitor N3 hemihydrate is a potent inhibitor of SARS-CoV-2 Mpro with an EC50 of 16.77 μM for SARS-CoV-2. Mpro inhibitor N3 hemihydrate specifically inhibits Mpro from multiple coronaviruses, including SARS-CoV and MERS-CoV. Mpro inhibitor N3 hemihydrate displays inhibition against HCoV-229E, FIPV, and MHV-A59 with individual IC50 of 4.0 μM, 8.8 μM, and 2.7 μM, respectively.
|
-
- HY-13803C
-
|
Tazemetostat hydrobromide
EPZ-6438 hydrobromide; E-7438 hydrobromide
|
Histone Methyltransferase
|
Cancer
|
|
Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC50 of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
|
-
- HY-122862
-
|
RAS inhibitor Abd-7
|
Ras
|
Cancer
|
|
RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V.
|
-
- HY-P1290A
-
|
PKA Inhibitor Fragment (6-22) amide TFA
PKI-(6-22)-amide TFA
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-B0166
-
-
- HY-P0222
-
|
PKI(5-24)
|
PKA
|
Others
|
|
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
|
-
- HY-114996
-
-
- HY-103032
-
|
Multi-kinase inhibitor 1
|
PDGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.
|
-
- HY-Y0445A
-
|
Sodium dichloroacetate
|
PDHK
Reactive Oxygen Species
NKCC
Apoptosis
|
Cancer
|
|
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
|
-
- HY-66005
-
-
- HY-13512
-
|
Camostat mesylate
Camostat mesilate; FOY305; FOY-S980
|
Ser/Thr Protease
SARS-CoV
|
Infection
Inflammation/Immunology
|
|
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase.
|
-
- HY-122632
-
|
Ciliobrevin D
|
Hedgehog
|
Cancer
|
|
Ciliobrevin D is a cell-permeable, reversible and specific inhibitor of AAA+ ATPase motor cytoplasmic dynein. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation. Ciliobrevin D inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.
|
-
- HY-16594
-
|
Lactacystin
|
Proteasome
|
Neurological Disease
|
|
Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces neurite outgrowth.
|
-
- HY-B0166A
-
|
L-Ascorbic acid sodium salt
Sodium L-ascorbate; Vitamin C sodium salt
|
Calcium Channel
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.
|
-
- HY-135391
-
-
- HY-15233
-
|
Letermovir
AIC246
|
CMV
|
Infection
|
|
Letermovir (AIC246) is a potent inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
|
-
- HY-50909
-
|
Perifosine
KRX-0401; NSC 639966; D21266
|
Akt
Autophagy
Apoptosis
|
Cancer
|
|
Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
|
-
- HY-101766
-
-
- HY-16510A
-
-
- HY-N0143
-
|
Phlorizin
Floridzin; NSC 2833
|
SGLT
Na+/K+ ATPase
|
Metabolic Disease
|
|
Phlorizin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na +/K +-ATPase inhibitor.
|
-
- HY-U00096
-
-
- HY-B1243
-
-
- HY-32351
-
-
- HY-N7089
-
|
Benzoyleneurea
|
Bacterial
|
Infection
|
|
Benzoyleneurea possesses anti-bacterial activity. Benzoyleneurea scaffold can be used in the synthesis of novel protein geranylgeranyltransferase-I (PGGTase-I) inhibitors.
|
-
- HY-18931A
-
|
NSC305787 hydrochloride
|
Others
|
Cancer
|
|
NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
|
-
- HY-15247
-
-
- HY-16510
-
-
- HY-12357
-
-
- HY-101464
-
|
ML329
|
Others
|
Others
|
|
ML329 is a micropthalmia-associated transcription factor (MITF) inhibitor, which inhibits TRPM-1 promoter activity with an IC50 of 1.2 μM.
|
-
- HY-12682
-
|
Glutaminase C-IN-1
Compound 968
|
Glutaminase
|
Cancer
|
|
Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
|
-
- HY-102007A
-
|
Gamitrinib TPP hexafluorophosphate
|
HSP
|
Cancer
|
|
Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
|
-
- HY-100541
-
|
INH6
|
Apoptosis
|
Cancer
|
|
INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC50 of 2.4 μM.
|
-
- HY-32351A
-
-
- HY-100735
-
-
- HY-13067
-
-
- HY-15679
-
-
- HY-19352
-
-
- HY-107433
-
-
- HY-126134
-
-
- HY-18931
-
|
NSC305787
|
Others
|
Cancer
|
|
NSC305787 is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
|
-
- HY-15223
-
-
- HY-15457
-
-
- HY-100792
-
|
URB602
|
Others
|
Cancer
|
|
URB602 is a selective monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL with IC50 of 28±4 μM through a noncompetitive mechanism.
|
-
- HY-112164
-
-
- HY-N7452
-
-
- HY-19763
-
|
BEBT-908
PI3Kα inhibitor 1
|
PI3K
|
Cancer
|
|
BEBT-908 (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC50<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC50≤1 μM) .
|
-
- HY-18979
-
|
Lactimidomycin
|
Influenza Virus
|
Cancer
Infection
|
|
Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities.
|
-
- HY-N0149
-
-
- HY-100263
-
-
- HY-N0342
-
-
- HY-101244
-
-
- HY-112870A
-
-
- HY-P0290A
-
-
- HY-23460A
-
|
4-Ethynyl-L-phenylalanine hydrochloride
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
4-Ethynyl-L-phenylalanine hydrochloride is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine hydrochloride is a competitive inhibitor with regard to the substrate tryptophan, with a Ki of 32.6 μM. 4-Ethynyl-L-phenylalanine hydrochloride selectively and reversibly inhibits the biosynthesis of serotonin.
|
-
- HY-103194
-
|
KH7
|
Others
|
Others
|
|
KH7 is a soluble adenylyl cyclase (sAC)-specific inhibitor, with IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.
|
-
- HY-23460
-
|
4-Ethynyl-L-phenylalanine
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
4-Ethynyl-L-phenylalanine is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine is a competitive inhibitor with regard to the substrate tryptophan, with a Ki of 32.6 μM. 4-Ethynyl-L-phenylalanine selectively and reversibly inhibits the biosynthesis of serotonin.
|
-
- HY-P1376A
-
|
G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
|
|
G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-133114
-
-
- HY-W006230
-
|
Anthraflavic acid
|
Others
|
Cancer
|
|
Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.
|
-
- HY-118532
-
|
Tyrphostin AG30
AG30
|
EGFR
|
Cancer
|
|
Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.
|
-
- HY-11001
-
|
PHA-793887
|
CDK
Apoptosis
|
Cancer
|
|
PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.
|
-
- HY-100222
-
|
CZ415
|
mTOR
|
Cancer
|
|
CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.
|
-
- HY-119692
-
|
Curvulin
|
Microtubule/Tubulin
|
Others
|
|
Curvulin, isolated from Curvularia lunata, is a phytotoxin. Curvularin is reported to inhibit microtubule assembly and has also been shown to inhibit iNOS expression.
|
-
- HY-12056
-
|
BIX02189
|
MEK
ERK
|
Cancer
|
|
BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
|
-
- HY-12957
-
-
- HY-10367A
-
|
Canertinib dihydrochloride
CI-1033 dihydrochloride; PD-183805 dihydrochloride
|
EGFR
|
Cancer
|
|
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
|
-
- HY-135383
-
-
- HY-12204
-
|
PFK-015
|
Autophagy
|
Cancer
|
|
PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.
|
-
- HY-100750
-
-
- HY-13577A
-
|
Oclacitinib maleate
PF-03394197 maleate
|
JAK
|
Inflammation/Immunology
|
|
Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC50=10 nM).
|
-
- HY-N3002
-
|
α-Arbutin
4-Hydroxyphenyl α-D-glucopyranoside
|
Tyrosinase
|
Metabolic Disease
|
|
α-Arbutin (4-Hydroxyphenyl α-D-glucopyranoside) is emerging as popular and effective skin whiteners, acting as tyrosinase inhibitor.
|
-
- HY-111357
-
|
Antifungal agent 2
|
Fungal
|
Infection
|
|
Antifungal agent 2 is a broad-spectrum fungal inhibitor which inhibits growth of pertinent species of Candida, Cryptococcus, and Aspergillus at a concentration as low as 0.5 μg/mL.
|
-
- HY-13966
-
|
2-Deoxy-D-glucose
2-DG; 2-Deoxy-D-arabino-hexose; D-Arabino-2-deoxyhexose
|
Hexokinase
HSV
Apoptosis
|
Cancer
|
|
2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase.
|
-
- HY-12589
-
-
- HY-126482
-
|
Telomerase-IN-2
|
Telomerase
|
Cancer
|
|
Telomerase-IN-2 is a telomerase inhibitor, and inhibits telomerase activity by decreasing expression of dyskerin, with an IC50 of 0.89 µM. Anti-cancer activity.
|
-
- HY-15162A
-
-
- HY-15417
-
|
ML-7 hydrochloride
|
Myosin
YAP
|
Cancer
|
|
ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC50=300 nM). ML-7 hydrochloride also inhibits YAP/TAZ.
|
-
- HY-12622
-
|
HSP70-IN-1
|
HSP
|
Cancer
|
|
HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
|
-
- HY-112861A
-
-
- HY-12444
-
|
Y15
FAK Inhibitor 14
|
FAK
|
Cancer
|
|
Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
|
-
- HY-100852
-
-
- HY-12289A
-
|
Defactinib hydrochloride
VS-6063 hydrochloride; PF 04554878 hydrochloride
|
FAK
|
Cancer
|
|
Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.
|
-
- HY-W018931
-
-
- HY-12589A
-
-
- HY-115666
-
|
COH34 analog 1
|
Others
|
Cancer
|
|
COH34 analog 1, a metabolite, is an oxidized analog of COH34. COH34 is a potent poly(ADP-ribose) glycohydrolase (PARG) inhibitor.
|
-
- HY-13806
-
|
XL388
|
mTOR
Autophagy
|
Cancer
|
|
XL388 is a highly potent and ATP-competitive mTOR inhibitor with an IC50 of 9.9 nM. XL388 simultaneously inhibits both mTORC1 and mTORC2.
|
-
- HY-12744
-
-
- HY-10129
-
|
Veliparib
ABT-888
|
PARP
Autophagy
|
Cancer
|
|
Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
|
-
- HY-111651
-
-
- HY-N5015
-
|
Rosmanol
|
Others
|
Inflammation/Immunology
Cancer
|
|
Rosmanol could inhibit the oxidation of low density lipoprotein (LPL) and significantly inhibit lipopolysaccharide induced iNOS and COX-2 expression, with anti-inflammatory effect.
|
-
- HY-133246
-
-
- HY-10366
-
-
- HY-112445
-
-
- HY-12479A
-
|
Epetraborole hydrochloride
GSK2251052 hydrochloride
|
Bacterial
|
Infection
|
|
Epetraborole hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor, which inhibits protein synthesis by binding "to the terminal adenosine ribose (A76) of leucyl-tRNA synthetase".
|
-
- HY-19832
-
|
SC66
|
Akt
Apoptosis
|
Cancer
|
|
SC66 is an Akt inhibitor, reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells.
|
-
- HY-136110
-
-
- HY-115584
-
|
Lufenuron
|
Parasite
|
Infection
|
|
Lufenuron is a lipophilic benzoylurea insecticide and a chitin synthesis inhibitor that can used for flea and fish lice control. Lufenuron inhibits moulting of arthropods.
|
-
- HY-N2182
-
-
- HY-100303
-
-
- HY-135328
-
-
- HY-126146
-
-
- HY-B1479C
-
-
- HY-112136
-
|
TAO Kinase inhibitor 1
|
Others
|
Cancer
|
|
TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death.
|
-
- HY-100374
-
|
Val-Cit-PAB-MMAE
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE (HY-15162). MMAE a potent mitotic inhibitor by inhibiting tubulin polymerization.
|
-
- HY-P0222A
-
|
PKI(5-24) TFA
|
PKA
|
Others
|
|
PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
|
-
- HY-B1479
-
-
- HY-50846
-
|
SCH772984
|
ERK
|
Cancer
|
|
SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
|
-
- HY-N0112
-
|
Dihydromyricetin
Ampelopsin; Ampeloptin
|
mTOR
Influenza Virus
DNA/RNA Synthesis
Autophagy
|
Cancer
Infection
|
|
Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
|
-
- HY-15480
-
|
NSC 42834
JAK2 Inhibitor V; Z3
|
JAK
|
Cancer
|
|
NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
|
-
- HY-B1479B
-
-
- HY-100126
-
|
Tubercidin
7-Deazaadenosine
|
Bacterial
DNA/RNA Synthesis
Influenza Virus
Antibiotic
|
Infection
|
|
Tubercidin (7-Deazaadenosine) is an antibiotic obtained from Streptomyces tubercidicus. Tubercidin inhibits the growth of Streptococcus faecalis (8043) with an IC50 of 0.02 μM. Tubercidin inhibits polymerases by incorporating DNA or RNA, thereby inhibiting DNA replication, RNA and protein synthesis. Tubercidin is a weak inhibitor of adenosine phosphorylase, and interferes with the phosphorylation of adenosine and AMP. Tubercidin has antiviral activity.
|
-
- HY-B0968A
-
|
Trimetazidine
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-15463
-
|
Imatinib
STI571; CGP-57148B
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
|
Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
|
-
- HY-110100
-
|
CPYPP
|
Others
|
Inflammation/Immunology
|
|
CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2 DHR-2 for Rac1 in a dose-dependent manner with an IC50 of 22.8 µM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9.
|
-
- HY-112701
-
|
CCR6 inhibitor 1
|
CCR
|
Cancer
Inflammation/Immunology
Endocrinology
|
|
CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer.
|
-
- HY-B0968
-
|
Trimetazidine dihydrochloride
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-B0879A
-
|
Suramin sodium salt
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
Parasite
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- HY-B0879
-
-
- HY-100434
-
|
PD-161570
|
FGFR
PDGFR
EGFR
Src
TGF-β Receptor
|
Cancer
Cardiovascular Disease
|
|
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
|
-
- HY-12041
-
|
SP600125
|
JNK
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 inhibits autophagy and activates apoptosis.
|
-
- HY-N2360
-
|
Hinokiflavone
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity.
|
-
- HY-122727
-
|
STL127705
|
DNA-PK
|
Cancer
|
|
STL127705 (Compound L) is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5 μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC50, 2.5 μM).
|
-
- HY-113957
-
|
MPI_5a
|
HDAC
|
Cancer
|
|
MPI_5a is a potent and selective HDAC6 inhibitor (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM.
|
-
- HY-N2150
-
|
Psammaplin A
|
HDAC
DNA Methyltransferase
DNA/RNA Synthesis
Bacterial
|
Cancer
Infection
|
|
Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity.
|
-
- HY-18707
-
-
- HY-101938
-
-
- HY-15769A
-
-
- HY-19762
-
-
- HY-16511
-
|
Upamostat
WX-671
|
Ser/Thr Protease
PAI-1
|
Cancer
|
|
Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
|
-
- HY-14754
-
|
Salirasib
S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS
|
Ras
Autophagy
|
Cancer
|
|
Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
|
-
- HY-101873
-
-
- HY-70035
-
|
Otamixaban
FXV673
|
Factor Xa
|
Cardiovascular Disease
|
|
Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.
|
-
- HY-107643
-
|
Reversan
CBLC4H10
|
P-glycoprotein
|
Cancer
|
|
Reversan (CBLC4H10) is a potent and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor.
|
-
- HY-100737
-
|
ML349
|
Phospholipase
|
Cancer
|
|
ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
|
-
- HY-50714
-
|
Quiflapon sodium
MK-591 sodium
|
FLAP
Apoptosis
|
Inflammation/Immunology
|
|
Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
|
-
- HY-103334
-
-
- HY-18729A
-
|
L-NAME hydrochloride
NG-Nitroarginine methyl ester hydrochloride
|
NO Synthase
|
Cancer
|
|
L-NAME hydrochloride inhibits NOS with an IC50 of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC50 value of 1.4 μM.
|
-
- HY-B0069
-
-
- HY-16214
-
|
FX-11
LDHA Inhibitor FX11
|
Lactate Dehydrogenase
|
Cancer
|
|
FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 23.3 μM for HeLa cell，a Ki value of 8 μM.
|
-
- HY-12055
-
|
BIX02188
|
MEK
ERK
|
Cancer
|
|
BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.
|
-
- HY-100891
-
-
- HY-15248
-
|
GDC-0349
|
mTOR
Autophagy
|
Cancer
|
|
GDC-0349 is a potent and selective ATP-competitive mTOR inhibitor with a Ki of 3.8 nM. GDC-0349 inhibits of both mTORC1 and mTORC2 complexes.
|
-
- HY-17469
-
|
Gimeracil
Gimestat
|
Others
|
Cancer
|
|
Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD).
|
-
- HY-13327
-
|
Evacetrapib
LY2484595
|
CETP
|
Cardiovascular Disease
|
|
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.
|
-
- HY-N3266
-
|
Methyl rosmarinate
|
Tyrosinase
|
Cancer
|
|
Methyl rosmarinate is a noncompetitive tyrosinase inhibitor which is isolated from Rabdosia serra, with an IC50 of 0.28 mM for mushroom tyrosinase, and also inhibits a-glucosidase.
|
-
- HY-100965
-
-
- HY-33900
-
|
Dihydrofuran-3(2H)-one
3-Oxotetrahydrofuran
|
Others
|
Others
|
|
Dihydrofuran-3(2H)-one (3-Oxotetrahydrofuran) is used for synthesizing cyclic ketone inhibitors that inhibits the serine protease plasmin.
|
-
- HY-15769
-
|
WHI-P180
Janex 3
|
VEGFR
EGFR
|
Cancer
|
|
WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
|
-
- HY-100562
-
-
- HY-15338
-
|
TG003
|
CDK
|
Cancer
|
|
TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
|
-
- HY-111621
-
|
DC661
|
Autophagy
Apoptosis
|
Cancer
|
|
DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor, inhibits autophagy, and acts as an anti-lysosomal agent. Anti-cancer activity.
|
-
- HY-12964
-
|
SGI-7079
|
TAM Receptor
|
Cancer
|
|
SGI-7079 is an Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 μM, respectively.
|
-
- HY-10165
-
|
PSI-6130
R 1656
|
HCV
|
Infection
|
|
PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM.
|
-
- HY-P1044
-
|
Spinorphin
LVV-hemorphin-4
|
Others
|
Neurological Disease
|
|
Spinorphin is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect.
|
-
- HY-135570
-
-
- HY-101587
-
-
- HY-101872
-
-
- HY-10005
-
|
Flavopiridol
HMR-1275; Alvocidib; L86-8275
|
CDK
Autophagy
HIV
|
Cancer
|
|
Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
|
-
- HY-111381
-
|
BI-3812
|
Bcl-2 Family
|
Cancer
|
|
BI-3812 is potent and efficacious BCL6 inhibitor, inhibiting the BTB domain of BCL6, with an IC50 of ≤3 nM; BI-3812 has antitumor activity.
|
-
- HY-12688
-
|
Succinyl phosphonate
|
Endogenous Metabolite
Reactive Oxygen Species
|
Neurological Disease
|
|
Succinyl phosphonate is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
|
-
- HY-N2553
-
|
4-Deoxypyridoxine 5'-phosphate
|
LPL Receptor
|
Metabolic Disease
|
|
4-Deoxypyridoxine 5'-phosphate is a Pyridoxal 5'-phosphate analogue and a sphingosine 1-phosphate (S1P) inhibitor. 4-Deoxypyridoxine 5'-phosphate inhibits ornithine decarboxylase activity with a Ki of 60 μM. 4-Deoxypyridoxine 5'-phosphate is a competitive inhibitor of the activation of glutamate apodecarboxylase by Pyridoxal 5'-phosphate (Ki of 0.27 μM) and strongly inhibits glutamate-dependent labeling of glutamate decarboxylase.
|
-
- HY-15509A
-
|
Semapimod tetrahydrochloride
CNI-1493; CPSI-2364 tetrahydrochloride
|
TNF Receptor
Interleukin Related
p38 MAPK
|
Inflammation/Immunology
|
|
Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders.
|
-
- HY-112504
-
-
- HY-B1480
-
-
- HY-17479A
-
-
- HY-19819
-
-
- HY-A0063A
-
-
- HY-U00208
-
-
- HY-19649
-
-
- HY-112502B
-
-
- HY-N0274
-
-
- HY-112502
-
|
MethADP
Adenosine 5'-(α,β-methylene)diphosphate
|
CD73
|
Cancer
|
|
MethADP is a specific CD73 inhibitor.
|
-
- HY-15759A
-
-
- HY-17620
-
-
- HY-U00065
-
-
- HY-112504A
-
-
- HY-124756
-
|
SBI-425
|
Phosphatase
|
Cardiovascular Disease
|
|
SBI-425 is a potent, selective and oral bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor. Long-term administration of SBI-425 effectively reaches and inhibits TNAP in the vasculature, improving cardiovascular parameters and survival at a dose that does not cause a detectable change in bone.
|
-
- HY-12842
-
|
UC-112
|
IAP
|
Cancer
|
|
UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).
|
-
- HY-B0789
-
|
SU6656
|
Src
FAK
Akt
|
Cancer
|
|
SU6656 is a Src family kinases inhibitor with IC50s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.
|
-
- HY-106697
-
|
Statil
Ponalrestat
|
Aldose Reductase
|
Metabolic Disease
|
|
Statil (Ponalrestat) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Statil selectively inhibits ALR2 (Ki=7.7 nM) over ALR1 (Ki=60 μM). Statil inhibits the conversion of glucose to sorbitol.
|
-
- HY-108486
-
|
Herbimycin A
|
Bacterial
Antibiotic
|
|
|
Herbimycin A, an ansamycin antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60 v-src and p210 BCR-ABL. Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.
|
-
- HY-13803
-
|
Tazemetostat
EPZ-6438; E-7438
|
Histone Methyltransferase
|
Cancer
|
|
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.
|
-
- HY-100111
-
-
- HY-111409
-
-
- HY-12871C
-
|
Atuveciclib S-Enantiomer
BAY-1143572 S-Enantiomer
|
CDK
|
Cancer
|
|
Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is a potent and selective CDK9 inhibitor, which inhibits CDK9/CycT1 with an IC50 of 16 nM.
|
-
- HY-B0856
-
|
Validamycin A
|
Fungal
Tyrosinase
|
Infection
|
|
Validamycin A is an aminoglycoside agricultural antibiotic. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL. Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM.
|
-
- HY-13012
-
|
RepSox
E-616452; SJN 2511
|
TGF-β Receptor
|
Cancer
|
|
RepSox (E-616452) is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC50 of 4 nM.
|
-
- HY-W011044
-
|
CID 5951923
|
KLF
|
Cancer
|
|
CID 5951923 is a potent inhibitor of Krüppel-like factor 5 (KLF5), with an IC50 of 603 nM. CID 5951923 can inhibit proliferation of cancer cells in vitro.
|
-
- HY-19363
-
-
- HY-13991
-
|
CCG-1423
|
Ras
|
Cancer
|
|
CCG-1423 is a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis.
|
-
- HY-50866
-
-
- HY-124861
-
-
- HY-16667
-
|
HLM006474
|
Others
|
Cancer
|
|
HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
|
-
- HY-19696A
-
|
Tauroursodeoxycholate Sodium
Sodium tauroursodeoxycholate; Tauroursodeoxycholic acid sodium salt
|
ERK
Caspase
|
Cancer
|
|
Tauroursodeoxycholate Sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
|
-
- HY-14605BS
-
-
- HY-15881
-
|
TCS JNK 5a
JNK Inhibitor IX
|
JNK
Apoptosis
|
Cancer
|
|
TCS JNK 5a is a potent JNK3 inhibitor with a pIC50 of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC50 of 6.5.
|
-
- HY-13227
-
|
SD-208
|
TGF-β Receptor
|
Cancer
|
|
SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
|
-
- HY-15125
-
-
- HY-14682
-
|
GSK319347A
|
IKK
|
Inflammation/Immunology
|
|
GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM.
|
-
- HY-13648
-
|
Incyclinide
CMT-3; COL-3
|
MMP
|
Cancer
|
|
Incyclinide (CMT-3, COL-3) is a matrix metalloproteinase (MMP) inhibitor, thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis.
|
-
- HY-15192
-
|
GSK 650394
|
SGK
Influenza Virus
|
Cancer
Infection
|
|
GSK 650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. GSK 650394 also inhibits influenza virus replication.
|
-
- HY-15719
-
|
NU 7026
LY293646
|
DNA-PK
Apoptosis
|
Cancer
|
|
NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.
|
-
- HY-12993
-
|
RSV604
(S)-1-(2-Fluorophenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea
|
RSV
|
Infection
|
|
RSV604 is a novel inhibitor of respiratory syncytial virus replication(EC50=0.86 uM); a putative RSV nucleoprotein(N) inhibitor in phase 2 clinical trials.
|
-
- HY-B0869A
-
|
Bispyribac sodium
|
Others
|
Others
|
|
Bispyribac sodium is a selective, systemic and post emergent herbicide used to eradicate grasses and broad leaf weeds. Bispyribac sodium is also an acetolactate synthase (ALS or known as AHAS) inhibitor.
|
-
- HY-13915
-
|
NSC348884
|
Apoptosis
|
Cancer
|
|
NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.
|
-
- HY-112522
-
|
HS79
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
HS-79 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-79 is able to inhibit the incorporation of tritiated acetate into lipids with an IC50 of 1.57 μM.
|
-
- HY-16663
-
|
ITX3
|
Others
|
Others
|
|
ITX3 is a specific and nontoxic inhibitor of the TrioN (N-terminal GEF domain of the multidomain Trio protein) with IC50 of 76 uM; inhibits TrioN-stimulated RhoG exchange in vitro.
|
-
- HY-100223
-
-
- HY-W009783
-
|
1-Deoxymannojirimycin hydrochloride
|
HIV
Influenza Virus
|
Infection
|
|
1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits HIV‐1 strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity.
|
-
- HY-B0167A
-
-
- HY-101920
-
|
Autophinib
|
Autophagy
|
Cancer
Neurological Disease
|
|
Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34.
|
-
- HY-N1127
-
|
Tricin
|
CMV
|
Cancer
Infection
|
|
Tricin is a natural flavonoid present in large amounts in rice bran. Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7.
|
-
- HY-W011094
-
|
Win 18446
|
Aldehyde Dehydrogenase (ALDH)
|
Endocrinology
|
|
Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC50 of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes.
|
-
- HY-N2532
-
|
Diphyllin
|
HIV
Proton Pump
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
|
|
Diphyllin is an arylnaphthalene lignan isolated from Justicia procumbens and is a potent HIV-1 inhibitor with an IC50 of 0.38 μM. Diphyllin is active against vesicular stomatitis virus (VSV) and influenza virus. Diphyllin is a vacuolar type H +-ATPase (V-ATPase) inhibitor with an IC50 value of 17 nM and inhibits lysosomal acidification in human osteoclasts. Diphyllin inhibits NO production with an IC50 of 50 μM and has anticancer and anti-inflammatory activities.
|
-
- HY-115510
-
|
SPR inhibitor 3
SPRi3
|
Others
|
Inflammation/Immunology
|
|
SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels.
|
-
- HY-12276
-
|
MALT1 inhibitor MI-2
|
MALT1
|
Cancer
|
|
MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals.
|
-
- HY-14521
-
|
Lometrexol
DDATHF
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-131275
-
|
Imatinib Impurity E
|
Others
|
Others
|
|
Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
|
-
- HY-14521B
-
|
Lometrexol hydrate
DDATHF hydrate
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-N6701
-
|
Dihydrocytochalasin B
|
Arp2/3 Complex
|
Cancer
|
|
Dihydrocytochalasin B (H2CB) is a Cytokinesis inhibitor and changes the morphology of the cells, similar to that of cytochalasin B; does not inhibit glucose transport. Dihydrocytochalasin B (H2CB) disrupts the actin structure and inhibits the ability of growth factors to stimulate DNA synthesis, reversibly blocks initiation of DNA synthesis. Dihydrocytochalasin B (H2CB) inhibits active calcium transport and causes a Ca 2+increase in the mucosal scrapings.
|
-
- HY-12688A
-
|
Succinyl phosphonate trisodium salt
|
Endogenous Metabolite
Reactive Oxygen Species
|
Cancer
Metabolic Disease
Neurological Disease
|
|
Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
|
-
- HY-B1320
-
|
Meclofenamate sodium
Meclofenamic acid sodium
|
Gap Junction Protein
|
Inflammation/Immunology
|
|
Meclofenamic acid sodium is a nonsteroidal anti-inflammatory drug (NSAID) approved for use in arthritis (osteo and rheumatoid), analgesia (mild to moderate pain), dysmenorrhea, and heavy menstrual blood loss (menorrhagia). Meclofenamic acid sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor.
|
-
- HY-N5011
-
|
5,7-Dimethoxyflavone
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
|
|
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor.
|
-
- HY-103710
-
|
IBR2
|
RAD51
Apoptosis
|
Cancer
|
|
IBR2 is a potent and specific RAD51 inhibitor and inhibits RAD51-mediated DNA double-strand break repair. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, inhibits cancer cell growth and induces apoptosis.
|
-
- HY-N7204
-
-
- HY-111549
-
|
Bragsin1
|
Others
|
Cancer
|
|
Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity.
|
-
- HY-17401
-
|
Ranolazine dihydrochloride
CVT 303 dihydrochloride; RS 43285
|
Calcium Channel
Sodium Channel
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor.
|
-
- HY-13982
-
|
JSH-23
|
NF-κB
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation.
|
-
- HY-W009156
-
-
- HY-13599
-
|
Cladribine
2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA
|
Adenosine Deaminase
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Cladribine (2CdA), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity and can be used for the research of several hematologic malignancies and multiple sclerosis.
|
-
- HY-125586
-
|
β-Amanitin
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
|
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
|
-
- HY-11006
-
|
KU-57788
NU7441
|
DNA-PK
CRISPR/Cas9
|
Cancer
|
|
KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC50 of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC50s of 5.0 and 1.7 μM, respectively.
|
-
- HY-14644A
-
|
Apilimod mesylate
STA 5326 mesylate
|
Interleukin Related
PIKfyve
|
Inflammation/Immunology
|
|
Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. Apilimod is a potent and highly selective PIKfyve inhibitor.
|
-
- HY-129769
-
|
CMLD012073
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
CMLD012073 is an amidino-rocaglates and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012073 inhibits the growth of NIH/3T3 cells with an IC50 of 10 nM. CMLD012073 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A).
|
-
- HY-136199
-
|
SIRT1-IN-1
|
Sirtuin
CMV
|
Infection
|
|
SIRT1-IN-1 is a selective SIRT1 inhibitor with an IC50 of 0.205 μM. SIRT1-IN-1 inhibits SIRT2 with an IC50 of 11.5 μM. SIRT1-IN-1, a indole, is a cytomegalovirus (CMV) inhibitors and has antiviral activity.
|
-
- HY-108900
-
|
Leu-AMS
|
Aminoacyl-tRNA Synthetase
Bacterial
|
Cancer
Infection
|
|
Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria.
|
-
- HY-B0182
-
|
Carmofur
HCFU
|
Nucleoside Antimetabolite/Analog
SARS-CoV
Virus Protease
|
Cancer
|
|
Carmofur (HCFU), a derivative of 5-Fluorouracil, is an antineoplastic agent. Carmofur is an inhibitor of acid ceramidase with an IC50 of 79 nM for the rat enzyme. Carmofur inhibits the SARS-CoV-2 main protease (Mpro). Carmofur Inhibits SARS-CoV-2 in Vero E6 cell with an EC50 of 24.3 μM.
|
-
- HY-14644
-
|
Apilimod
STA 5326
|
Interleukin Related
PIKfyve
|
Inflammation/Immunology
|
|
Apilimod (STA 5326) is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. Apilimod is a potent and highly selective PIKfyve inhibitor.
|
-
- HY-N2036
-
|
Mosloflavone
|
Enterovirus
Bacterial
|
Infection
|
|
Mosloflavone is a flavonoid isolated from Scutellaria baicalensis Georgi with anti-EV71 activity. Mosloflavone inhibits VP2 virus replication and protein expression during the initial stage of virus infection and inhibits viral VP2 capsid protein synthesis. Mosloflavone is a promising biocide and inhibits P. aeruginosa virulence and biofilm formation.
|
-
- HY-108341A
-
|
PF-06424439 methanesulfonate
|
Acyltransferase
|
Metabolic Disease
|
|
PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
|
-
- HY-15982
-
-
- HY-W015445
-
|
SD-169
|
p38 MAPK
|
Metabolic Disease
|
|
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
|
-
- HY-117889
-
|
PARP14 inhibitor H10
|
PARP
Apoptosis
|
Cancer
|
|
PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (≈24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis.
|
-
- HY-B1099
-
|
Hycanthone
|
DNA/RNA Synthesis
Topoisomerase
Parasite
|
Infection
|
|
Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.
|
-
- HY-110150
-
|
UNC3230
|
Others
|
Cancer
Inflammation/Immunology
|
|
UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects.
|
-
- HY-18643
-
|
TZ9
|
E1/E2/E3 Enzyme
|
Cancer
|
|
TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.
|
-
- HY-18696
-
|
AMG-337
|
c-Met/HGFR
|
Cancer
|
|
AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays.
|
-
- HY-P2502
-
-
- HY-10006
-
|
Flavopiridol Hydrochloride
Alvocidib Hydrochloride; L86-8275 Hydrochloride; HMR-1275 Hydrochloride
|
CDK
Autophagy
HIV
|
Cancer
|
|
Flavopiridol Hydrochloride (Alvocidib Hydrochloride) is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
|
-
- HY-N0102
-
-
- HY-11102
-
-
- HY-14427
-
-
- HY-13865
-
|
P 22077
|
Deubiquitinase
|
Cancer
|
|
P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. It also inhibits USP47 with an EC50 of 8.74 μM.
|
-
- HY-16712
-
|
LDN-214117
|
TGF-β Receptor
|
Cancer
|
|
LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).
|
-
- HY-15716
-
|
Kobe0065
|
Ras
Apoptosis
|
Cancer
|
|
Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
|
-
- HY-U00422
-
|
K-756
|
PARP
|
Cancer
|
|
K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TNKS1 and TNKS2 with IC50s of 31 and 36 nM, respectively.
|
-
- HY-100742
-
-
- HY-114166
-
-
- HY-101840
-
-
- HY-15004
-
|
AUZ 454
K03861
|
CDK
|
Cancer
|
|
AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
|
-
- HY-N6738
-
-
- HY-128726
-
-
- HY-19712
-
-
- HY-102087
-
|
JPM-OEt
|
Cathepsin
|
Cancer
|
|
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity.
|
-
- HY-50908
-
|
Ridaforolimus
MK-8669; Deforolimus; AP23573
|
mTOR
Autophagy
|
Cancer
|
|
Ridaforolimus (MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.
|
-
- HY-101840A
-
-
- HY-10074
-
-
- HY-13020
-
-
- HY-112433
-
|
NIK SMI1
|
NF-κB
|
Inflammation/Immunology
|
|
NIK SMI1 is a potent, selective NF-κB inducing kinase (NIK) inhibitor, which inhibits NIK-catalyzed hydrolysis of ATP to ADP with IC50 of 0.23±0.17 nM.
|
-
- HY-18988
-
|
ETC-159
ETC-1922159
|
Porcupine
Wnt
|
Cancer
|
|
ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
|
-
- HY-129700
-
-
- HY-124944
-
|
APS6-45
|
Ras
|
Cancer
|
|
APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.
|
-
- HY-18964
-
|
MG-101
Calpain inhibitor I; Ac-LLnL-CHO; ALLN
|
Proteasome
|
Cancer
|
|
MG-101 is a potent inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively.
|
-
- HY-12961A
-
-
- HY-19236
-
-
- HY-101835
-
-
- HY-B1839
-
-
- HY-B0207A
-
-
- HY-15681
-
-
- HY-112670
-
-
- HY-19123
-
-
- HY-U00222
-
-
- HY-B1542A
-
-
- HY-112097
-
-
- HY-U00176
-
-
- HY-N0221
-
-
- HY-U00175
-
-
- HY-10827
-
-
- HY-13061
-
-
- HY-15723A
-
-
- HY-66009
-
-
- HY-B0597
-
-
- HY-101644A
-
-
- HY-101647
-
-
- HY-12804
-
-
- HY-107362
-
-
- HY-101862
-
-
- HY-113057
-
-
- HY-12527
-
-
- HY-U00444
-
-
- HY-13555
-
|
β-Lapachone
ARQ-501; NSC-26326
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
|
β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.
|
-
- HY-17393
-
-
- HY-13728A
-
|
(R)-Plevitrexed
(R)-ZD 9331; (R)-BGC9331
|
Others
|
Cancer
|
|
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor.
|
-
- HY-100578
-
|
AGK2
|
Sirtuin
Apoptosis
|
Cancer
|
|
AGK2 is a selective SIRT2 inhibitor with an IC50 of 3.5 μM. AGK2 inhibits SIRT1 and SIRT3 with IC50s of 30 and 91 μM, respectively.
|
-
- HY-108318
-
-
- HY-112220
-
|
VIT-2763
|
Others
|
Metabolic Disease
|
|
VIT-2763, an oral ferroportin inhibitor, inhibits hepcidin binding to ferroportin and blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia.
|
-
- HY-16134A
-
|
Celgosivir hydrochloride
MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride
|
Glucosidase
HCV
HIV
|
Infection
|
|
Celgosivir hydrochloride (MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
|
-
- HY-107366
-
|
SGN-2FF
|
Others
|
Cancer
|
|
SGN-2FF is a potent and orally active inhibitor of fucosylation, directly inhibits fucosyltransferase activity. SGN-2FF possesses antitumor activity.
|
-
- HY-13605
-
-
- HY-113950
-
-
- HY-16956
-
|
CC-223
|
mTOR
Apoptosis
|
Cancer
|
|
CC-223 is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. CC-223 inhibits both mTORC1 and mTORC2.
|
-
- HY-14908
-
-
- HY-13605A
-
-
- HY-12558
-
|
LY3009120
DP-4978
|
Raf
Autophagy
|
Cancer
|
|
LY3009120 is a pan RAF inhibitor which inhibits BRAF V600E, BRAF WT and CRAF WT with IC50s of 5.8, 9.1 and 15 nM, respectively.
|
-
- HY-12990
-
|
Spautin-1
|
Autophagy
Apoptosis
|
Cancer
|
|
Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC50s of 0.6-0.7 μM.
|
-
- HY-100625
-
-
- HY-15871
-
|
GGTI298 Trifluoroacetate
|
Ras
Apoptosis
|
Cancer
|
|
GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM.
|
-
- HY-103028A
-
|
GSK963
|
RIP kinase
|
Others
|
|
GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro.
|
-
- HY-10241
-
|
Simeprevir
TMC435
|
HCV
HCV Protease
|
Infection
|
|
Simeprevir (TMC435) is an oral and potent HCV NS3/4A protease inhibitor with a Ki of 0.36 nM, and inhibits HCV replication with an EC50 of 7.8 nM.
|
-
- HY-P1291
-
|
PKI 14-22 amide,myristoylated
|
PKA
|
Cancer
|
|
PKI 14-22 amide,myristoylated is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
|
-
- HY-100437
-
|
HA15
|
HSP
Autophagy
Apoptosis
|
Cancer
|
|
HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.
|
-
- HY-10367
-
|
Canertinib
CI-1033; PD-183805
|
EGFR
|
Cancer
|
|
Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
|
-
- HY-N2403
-
|
Dihydrolycorine
|
Others
|
Neurological Disease
|
|
Dihydrolycorine is isolated from Lycoris radiate Herb with antihypertensive and neuroprotective activities. Dihydrolycorine is an inhibitor of protein synthesis in eukarytic cells by inhibiting the peptide bone formation step.
|
-
- HY-15283
-
|
Clopidogrel
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
|
-
- HY-125567
-
|
Antileukinate
|
CXCR
|
Inflammation/Immunology
|
|
Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury.
|
-
- HY-15518
-
|
LCL161
|
IAP
|
Cancer
|
|
LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.
|
-
- HY-17362
-
|
Vancomycin hydrochloride
|
Bacterial
Autophagy
Antibiotic
|
Infection
Cancer
|
|
Vancomycin hydrochloride is an antibiotic for the treatment of bacterial infections. It acts by inhibiting the second stage of cell wall synthesis of susceptible bacteria. Vancomycin also alters the permeability of the cell membrane and selectively inhibits ribonucleic acid synthesis.
|
-
- HY-12063
-
|
PHT-427
|
Akt
Apoptosis
|
Cancer
|
|
PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 µM and 5.2 µM and for Akt and PDPK1, respectively.
|
-
- HY-14177A
-
-
- HY-16134
-
|
Celgosivir
MBI 3253; MDL 28574; MX3253
|
Glucosidase
HCV
HIV
|
Infection
|
|
Celgosivir (MBI 3253; MDL 28574; MX3253) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
|
-
- HY-100395
-
|
F16
|
Apoptosis
|
Cancer
|
|
F16 is a potent growth inhibitor of the neu-overexpressing cells and also selectively inhibits proliferation of mammary epithelial as well as a variety of mouse mammary tumor and human breast cancer cell lines.
|
-
- HY-B0255
-
-
- HY-14177
-
|
B-Raf inhibitor 1
|
Raf
|
Cancer
|
|
B-Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
|
-
- HY-123523
-
-
- HY-13235
-
-
- HY-115537
-
|
NAE-IN-M22
|
Apoptosis
|
Cancer
|
|
NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
|
-
- HY-12305
-
|
Q-VD-OPh
QVD-OPH; Quinoline-Val-Asp-Difluorophenoxymethylketone
|
Caspase
HIV
|
Cancer
Infection
|
|
Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.
|
-
- HY-B0146
-
|
Verteporfin
CL 318952
|
YAP
Apoptosis
Autophagy
|
Cancer
|
|
Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis. Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation.
|
-
- HY-P1382
-
|
Rac1 Inhibitor W56
|
Ras
|
|
|
Rac1 Inhibitor W56 is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.
|
-
- HY-121750
-
|
CCG-222740
|
Ras
ROCK
|
Cancer
|
|
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.
|
-
- HY-129241
-
|
AGX51
|
Others
|
Cancer
|
|
AGX51 is a first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability. AGX51 inhibits pathologic ocular neovascularization.
|
-
- HY-103353
-
|
SID 26681509
|
Cathepsin
Parasite
|
Cancer
Infection
|
|
SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.
|
-
- HY-B0280
-
|
Ranolazine
CVT 303; RS 43285-003
|
Sodium Channel
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor.
|
-
- HY-10585A
-
|
Valproic acid sodium salt
Sodium Valproate
|
HDAC
Autophagy
Mitophagy
HIV
Notch
|
Cancer
|
|
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
|
-
- HY-13737
-
|
R1530
|
VEGFR
FGFR
Apoptosis
|
Cancer
|
|
R1530 is a highly potent, orally bioavailable, dual-acting mitosis/angiogenesis inhibitor, with antitumor and anti-angiogenic activity. R1530 is a multikinase inhibitor which binds to 31 kinases with Kds of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50s of 10 nM and 28 nM, respectively.
|
-
- HY-18944
-
|
FIT-039
|
CDK
HSV
CMV
DNA/RNA Synthesis
|
Infection
|
|
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
|
-
- HY-131011
-
|
Furanone C-30
|
Bacterial
|
|
|
Furanone C-30 is a synthetic furanone bacterial quorum sensing inhibitor. Furanone C-30 inhibits virulence factor expression in Pseudomonas aeruginosa and increases bacterial susceptibility to antibiotics in vitro.
|
-
- HY-13802
-
|
SC-514
GK 01140
|
IKK
|
Cancer
|
|
SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
|
-
- HY-12983
-
|
ALS-8112
|
RSV
|
Infection
|
|
ALS-8112 is a potent and selective respiratory syncytial virus (RSV) polymerase inhibitor. The 5'-triphosphate form of ALS-8112 inhibits RSV polymerase with an IC50 of 0.02 μM.
|
-
- HY-130055
-
|
HQNO
|
Mitochondrial Metabolism
|
Infection
|
|
HQNO, secreted by P. aeruginosa, is a potent electron transport chain inhibitor with a Kd of 64 nM for complex III. HQNO is a potent inhibitor of mitochondrial NDH-2 in many species.
|
-
- HY-103236
-
|
NSC232003
|
E1/E2/E3 Enzyme
|
Cancer
|
|
NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.
|
-
- HY-15845
-
|
STF-083010
|
IRE1
|
Cancer
|
|
STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
|
-
- HY-15284
-
|
Prasugrel
PCR 4099
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-104010
-
|
Asciminib
ABL001
|
Bcr-Abl
|
Cancer
|
|
Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
|
-
- HY-129111
-
|
EACC
|
Autophagy
|
Infection
Neurological Disease
|
|
EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion.
|
-
- HY-111940
-
|
LUT014
|
Raf
|
Inflammation/Immunology
|
|
LUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, and developed to reduce dose-limiting acneiform lesions associated EGFR Inhibitors treatment. Extracted from patent WO 2019026065A2 .
|
-
- HY-101441
-
|
ST-193
|
Arenavirus
|
Infection
|
|
ST-193 is a potent broad-spectrum arenavirus inhibitor; inhibits Guanarito, Junin, Lassa and Machupo virus with IC50 values of 0.44, 0.62, 1.4 and 3.1 nM, respectively.
|
-
- HY-B1418
-
|
Tazobactam
CL-298741; YTR-830H
|
Bacterial
Antibiotic
|
Infection
|
|
Tazobactam is a beta Lactamase Inhibitor with antibacterial activity
Target: Antibacterial
Tazobactam is a pharmaceutical drug that inhibits the action of bacterial β-lactamases, especially those belonging to the SHV-1 and TEM groups.
|
-
- HY-119176
-
|
Oxyfluorfen
|
Others
|
Others
|
|
Oxyfluorfen is a pre- and post-emergence diphenyl ether herbicide to control annual broad-leaved and grass weeds. Oxyfluorfen is a protoporphyrinogen oxidase inhibitor and inhibits photosynthesis by blocking chlorophyll synthesis.
|
-
- HY-15754
-
-
- HY-101780
-
|
EDO-S101
Tinostamustine
|
HDAC
|
Cancer
|
|
EDO-S101 (Tinostamustine) is a pan HDAC inhibitor; inhibits HDAC6, HDAC1, HDAC2 and HDAC3 with IC50 values of 9 nM, 9 nM and 25 nM, respectively.
|
-
- HY-U00461
-
-
- HY-126382
-
|
Hesperidin methylchalcone
|
NF-κB
|
Inflammation/Immunology
|
|
Hesperidin methylchalcone (Hesperidin methyl chalcone) inhibits oxidative stress, cytokine production and NF-κB activation. Hesperidin methylchalcone inhibits inflammation and pain. Hesperidin methylchalcone exhibits vasoprotective activity.
|
-
- HY-P1095
-
-
- HY-112885B
-
|
nor-NOHA monoacetate
Nω-Hydroxy-nor-L-arginine monoacetate
|
Arginase
|
Metabolic Disease
|
|
nor-NOHA (Nω-Hydroxy-nor-L-arginine) monoacetate is a potent and selective arginase inhibitor. nor-NOHA monoacetate inhibits rat liver arginase with a Ki of 0.5 µM.
|
-
- HY-10453
-
|
Ixazomib
MLN2238
|
Proteasome
Autophagy
|
Cancer
|
|
Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
|
-
- HY-17376
-
-
- HY-102049
-
-
- HY-100690
-
|
NSC16168
|
Others
|
Cancer
|
|
NSC16168 is a specific inhibitor of ERCC1-XPF, with an IC50 value of 0.42 μM. NSC16168 inhibits DNA repair and potentiates CDDP efficacy in cancer.
|
-
- HY-123999
-
-
- HY-112182
-
|
UM-164
DAS-DFGO-II
|
Src
p38 MAPK
Autophagy
|
Cancer
|
|
UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
|
-
- HY-19502
-
|
Artemisone
Artemifone; BAY 44-9585
|
Parasite
CMV
|
Infection
|
|
Artemisone (Artemifone) is a potent and semi-synthetic antimalarial, inhibits P. falciparum strains, with a mean IC50 of 0.83 nM. Artemisone is also a potent inhibitor of human CMV.
|
-
- HY-111507
-
|
PDGFRα kinase inhibitor 1
|
PDGFR
|
Cancer
|
|
PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.
|
-
- HY-13809
-
|
BMS-833923
XL-139
|
Smo
Apoptosis
|
Cancer
|
|
BMS-833923 (XL-139) is an orally bioavailable small-molecule inhibitor of Smoothened with potential antineoplastic activity; inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM.
|
-
- HY-12846
-
|
CCT196969
|
Raf
|
Cancer
|
|
CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRaf V600E and CRAF with IC50s of 0.1, 0.04, and 0.01 μM, respectively.
|
-
- HY-N2065
-
|
Withaferin A
|
NF-κB
Ferroptosis
|
Cancer
Inflammation/Immunology
|
|
Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
|
-
- HY-15704
-
|
LH846
|
Casein Kinase
|
Cancer
|
|
LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively.
|
-
- HY-32219
-
|
T863
|
Acyltransferase
|
Metabolic Disease
|
|
T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.
|
-
- HY-B0114
-
|
Oxcarbazepine
GP 47680
|
Sodium Channel
|
Neurological Disease
|
|
Oxcarbazepine (GP 47680) inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM.
|
-
- HY-14622
-
|
Necrostatin 2
|
RIP kinase
|
Cancer
|
|
Necrostatin 2 is a potent necroptosis inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM.
Necrostatin 2 is also a RIPK1 inhibitor.
|
-
- HY-B0631
-
|
Alendronic acid
|
Others
|
Cancer
|
|
Alendronic acid, a bisphosphonate, is a farnesyl diphosphate synthase (FDPS) inhibitor. Alendronic acid inhibits osteoclast-mediated bone resorption. Alendronic acid shows efficacy in postmenopausal osteoporosis, malignant hypercalcemia and Paget’s disease.
|
-
- HY-15284A
-
|
Prasugrel hydrochloride
PCR 4099 hydrochloride
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel hydrochloride (PCR 4099 hydrochloride), a thienopyridine and prodrug, inhibits platelet function. Prasugrel hydrochloride is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-18935A
-
|
CBL0137 hydrochloride
Curaxin-137 hydrochloride; CBL-C137 hydrochloride
|
MDM-2/p53
NF-κB
|
Cancer
|
|
CBL0137 hydrochloride is an inhibitor of the histone chaperone, FACT. CBL0137 hydrochloride can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 µM, respectively.
|
-
- HY-19530
-
|
PF-2771
|
Kinesin
|
Cancer
|
|
PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor, inhibiting CENP-E motor activity with an IC50 of 16.1 nM; PF-2771 is used as an anticancer agent.
|
-
- HY-108940
-
-
- HY-111505
-
-
- HY-19761
-
-
- HY-100580
-
|
Asaraldehyde
Asaronaldehyde; Asaraldehyde; 2,4,5-trimethoxy-Benzaldehyde
|
COX
|
Inflammation/Immunology
|
|
Asarylaldehyde is a natural COX-2 inhibitor, which isolated from carrot (Daucus carota L.) seeds significantly inhibits cyclooxygenase II (COX-2) activity at IC50 value 100 μg/mL.
|
-
- HY-103097
-
|
ST271
|
Phospholipase
|
Others
|
|
ST271 is a potent inhibitor of protein tyrosine kinase (PTK), inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF, with IC50s of 6.7 and 9 μM, respectively.
|
-
- HY-19541
-
-
- HY-12632
-
|
GNE 2861
|
PAK
|
Cancer
|
|
GNE 2861 is a PAK inhibitor that displays group II selectivity. GNE 2861 inhibits PAK4, PAK5 and PAK6 with IC50s of 7.5, 36, 126 nM, respectively.
|
-
- HY-101441A
-
|
ST-193 hydrochloride
|
Arenavirus
|
Infection
|
|
ST-193 hydrochloride is a potent broad-spectrum arenavirus inhibitor; inhibits Guanarito, Junin, Lassa and Machupo virus with IC50 values of 0.44, 0.62, 1.4 and 3.1 nM, respectively.
|
-
- HY-11101
-
-
- HY-101868
-
-
- HY-100639
-
-
- HY-100949
-
-
- HY-108314A
-
-
- HY-76299
-
-
- HY-B1083
-
-
- HY-128483
-
-
- HY-17003
-
-
- HY-101443
-
-
- HY-13518
-
-
- HY-B0544
-
-
- HY-B1581A
-
-
- HY-12242
-
-
- HY-15206
-
-
- HY-12242A
-
-
- HY-50865
-
-
- HY-B0134
-
-
- HY-B1413
-
-
- HY-B1194
-
-
- HY-19939S
-
-
- HY-U00217
-
-
- HY-100396
-
-
- HY-19756
-
-
- HY-U00313
-
-
- HY-Z0283
-
-
- HY-B2147
-
-
- HY-106024B
-
-
- HY-14252
-
-
- HY-P0290
-
-
- HY-N1187
-
-
- HY-101426
-
|
RG14620
Tyrphostin RG14620
|
EGFR
|
Cancer
|
|
RG14620 is an EGFR inhibitor with an IC50 of 3 μM.
|
-
- HY-A0022
-
-
- HY-B1847
-
-
- HY-101801
-
-
- HY-12991A
-
-
- HY-101703
-
